Patent Publication Number: US-8536097-B2

Title: 4-(4-haloalkyl-3-thiobenzoyl)pyrazoles and use thereof as herbicides

Description:
CROSS REFERENCE TO RELATED APPLICATIONS 
     This application claims priority to EP 10170238.9 filed Jul. 21, 2010, the content of which is incorporated herein by reference in its entirety. 
     BACKGROUND 
     1. Field of the Invention 
     The invention relates to the technical field of herbicides, more particularly that of herbicides for the selective control of broadleaf and grass weeds in crops of useful plants. 
     2. Description of Related Art 
     From various publications it is already known that certain benzoylpyrazoles possess herbicidal properties. For instance, EP 0 352 543, WO 00/03993, and WO 2008/125214 disclose benzoylpyrazoles substituted by various radicals. 
     The herbicidal activity of the compounds known from these publications, however, is frequently inadequate. It is therefore an object of the present invention to provide herbicidally active compounds whose herbicidal properties are improved as compared with those of the compounds known from the prior art. 
     SUMMARY 
     It has now been found that certain 4-benzoylpyrazoles whose phenyl ring carries a thio group in position 3 and a haloalkyl group in position 4 are especially suitable as herbicides. The present invention firstly provides 4-(4-haloalkyl-3-thiobenzoyl)pyrazoles of the formula (I) or salts thereof 
                         
in which
     X is (C 1 -C 4 )-alkyl,   Y is (C 1 -C 4 )-haloalkyl bar trifluoromethyl,   R 1  is (C 1 -C 4 )-alkyl,   R 2  is (C 1 -C 4 )-alkyl,   R 3  is hydrogen or (C 1 -C 4 )-alkyl,   R 4  is hydrogen, (C 1 -C 6 )-alkylsulfonyl, (C 1 -C 4 )-alkoxy-(C 1 -C 6 )-alkylsulfonyl, or is phenylsulfonyl, thiophenyl-2-sulfonyl, benzoyl, benzoyl-(C 1 -C 6 )-alkyl or benzyl, each of which is substituted by m identical or different radicals from the group consisting of halogen, (C 1 -C 4 )-alkyl, and (C 1 -C 4 )-alkoxy,   m is 0, 1, 2 or 3, and   n is 0, 1 or 2.   

    
    
     DETAILED DESCRIPTION OF A PREFERRED EMBODIMENT 
     Where R 4  is hydrogen, the compounds of the invention of the formula (I) may exist in the form of different tautomeric structures, depending on external conditions, such as solvent and pH, as follows: 
                         
Depending on the nature of the substituents, the compounds of the formula (I) contain an acidic proton which can be removed by reaction with a base. Examples of suitable bases include hydrides, hydroxides, and carbonates of lithium, sodium, potassium, magnesium, and calcium, and also ammonia and organic amines such as triethylamine and pyridine. In addition, salts may be formed by reaction with organic acids, such as formic acid or acetic acid, and with inorganic acids, such as phosphoric, hydrochloric or sulfuric acid. Such salts are likewise provided by the invention.
 
     In the formula (I) and all subsequent formulae, alkyl radicals having more than two carbon atoms may be straight-chain or branched. Alkyl radicals are, for example, methyl, ethyl, n- or iso-propyl, n-, iso-, tert- or 2-butyl, pentyl, hexyl, such as n-hexyl, iso-hexyl and 1,3-dimethylbutyl. Halogen is fluorine, chlorine, bromine or iodine. 
     Where a group is substituted multiply by radicals, this means that the group in question is substituted by one or more identical or different members from among the radicals specified. 
     Depending on the nature and attachment of the substituents, the compounds of the formula (I) may be present in the form of stereoisomers. Where, for example, one or more asymmetrically substituted carbon atoms or sulfoxides are present, then enantiomers and diastereomers may occur. Stereoisomers may be obtained from the mixtures resulting from the preparation process by customary separation methods, such as by chromatographic separation methods, for example. It is likewise possible for stereoisomers to be prepared selectively through deployment of stereoselective reactions using optically active starting materials and/or auxiliaries. The invention also relates to all of the stereoisomers and mixtures thereof that are embraced by the formula (I) but not defined specifically. 
     Of particular interest are compounds of the formula (I) in which
     X is (C 1 -C 4 )-alkyl,   Y is (C 1 -C 4 )-haloalkyl of bar trifluoromethyl,   R 1  is (C 1 -C 4 )-alkyl,   R 2  is (C 1 -C 4 )-alkyl,   R 3  is hydrogen or (C 1 -C 4 )-alkyl,   R 4  is hydrogen, (C 1 -C 6 )-alkylsulfonyl, (C 1 -C 4 )-alkoxy-(C 1 -C 6 )-alkylsulfonyl, or is phenylsulfonyl, thiophenyl-2-sulfonyl, benzoyl, benzoyl-(C 1 -C 6 )-alkyl or benzyl, each of which is substituted by m identical or different radicals from the group consisting of halogen, (C 1 -C 4 )-alkyl, and (C 1 -C 4 )-alkoxy,   m is 0, 1, 2 or 3, and   n is 0, 1 or 2.   

     Preference is given to compounds of the formula (I) in which
     X is (C 1 -C 4 )-alkyl,   Y is trichloromethyl, difluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl, pentafluoroethyl or heptafluoroisopropyl,   R 1  is (C 1 -C 4 )-alkyl,   R 2  is (C 1 -C 4 )-alkyl,   R 3  is hydrogen or (C 1 -C 4 )-alkyl,   R 4  is hydrogen, n-propylsulfonyl, methoxyethylsulfonyl, phenylsulfonyl, 4-methyl-phenylsulfonyl, or thiophenyl-2-sulfonyl, and   n is 0, 1 or 2.   

     Particular preference is given to compounds of the formula (I) in which
     X is methyl,   Y is difluoromethyl or pentafluoroethyl,   R 1  is methyl,   R 2  is methyl,   R 3  is hydrogen or methyl,   R 4  is hydrogen, and   n is 1 or 2.   

     Very particular preference is given to compounds of the formula (I) in which
     X is methyl,   Y is pentafluoroethyl,   R 1  is methyl,   R 2  is methyl,   R 3  is hydrogen or methyl,   R 4  is hydrogen, and   n is 1 or 2.   

     In all formulae given below, the substituents and symbols, unless defined otherwise, have the same meaning as described under formula (I). 
     Compounds of the invention in which R 4  is hydrogen may be prepared, for example, by the process, indicated in Scheme 1 and known from Acta Chem. Scand. 13 (1959), 1668-1670, by base-catalyzed reaction of a benzoyl halide (III) with a pyrazolone (II), or in accordance with the process indicated in Scheme 2 and known, for example, from EP-A 0 186 117, by base-catalyzed reaction of a benzoyl halide (III) with a pyrazolone (II) and subsequent rearrangement. These processes are also known from WO2005/122768. 
     
       
         
         
             
             
         
       
     
     
       
         
         
             
             
         
       
     
     The intermediate (IV) may also be prepared by direct reaction of a benzoic acid (IIIa) with a pyrazolone (II) with the addition of an activating condensation agent such as N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, for example. 
     Compounds of the invention in which R 4  has a definition other than hydroxyl are usefully prepared from the compounds obtainable in accordance with Scheme 1 or 2, by alkylation or acylation. Methods of this kind are fundamentally known to the skilled person and described in WO2005/122768, for example. 
     The pyrazolones of the formula (II) are available commercially or can be prepared in accordance with the process known to the skilled person and described in EP-A 240 001, for example. 
     The benzoyl halides of the formula (III) are prepared from the benzoic acids of the formula (IIIa) by means, for example, of reaction with thionyl chloride. 
     
       
         
         
             
             
         
       
     
     The benzoic acids (IIIa) are obtainable via a series of synthetic steps known per se to the skilled person. 
     For example, the synthesis of benzoic acids carrying a trifluoromethyl group as haloalkyl group in position 4 is known from WO 2008125214. Depending on the nature of the haloalkyl group, the processes described therein may be applied to the synthesis of the benzoic acids (IIIa). 
     A further possibility is the introduction of haloalkyl groups. For example, the introduction of a pentafluoroethyl group into position 4 of a benzonitrile is described in WO 2006/43064 and US 2007/185058. The benzonitrile may be converted subsequently into the corresponding benzoic acid (US 2007/185058). Also known is the substitution of the iodoaromatic compound by a haloalkyl group, a reaction which proceeds via the corresponding haloalkyl copper compound (A. A. Kolomeitsev et al., J. Org. Chem. 2008, 73 (7), 2607.). 
     Alternatively, haloalkyl groups may also be generated from other functional groups. A difluoromethyl group is accessible, for example, from the corresponding formyl group. A transformation of this kind is described for 4-formylbenzonitrile by C. P. Andrieux et. al. (Journal of the American Chemical Society 1997 (119), 40, 9527). The corresponding benzoic acid can then be generated from the product under basic conditions, for example (F. Mathey et. al., Tetrahedron 1975 (31), 391.). 
     Further possibilities for synthetic access to benzoic acids that may be applied to the synthesis of the benzoic acids (IIIa) are known from WO 03/014071. 
     The sulfur atom in position 3 of the benzoyl group need not necessarily be oxidized at the stage of the benzoic acid in order to generate compounds with n=1 or 2; for example, an oxidation of this kind at the stage of the enol ester or of the 4-benzoyl-5-hydroxypyrazole may also be useful. 
     Benzoic acids of the formula (IIIa) are new and likewise provided by the invention. 
     Collections of compounds of the formula (I) and/or salts thereof which can be synthesized by the aforementioned reactions can also be prepared in a parallel manner, it being possible for this to take place in a manual, partly automated or completely automated manner. In this connection, it is, for example, possible to automate the reaction procedure, the work-up or the purification of the products and/or intermediates. Overall, this is understood as meaning a procedure as described, for example, by D. Tiebes in Combinatorial Chemistry—Synthesis, Analysis, Screening (editor Gunther Jung), Verlag Wiley 1999, on pages 1 to 34. 
     For the parallel reaction procedure and work-up, it is possible to use a series of commercially available instruments, for example Calypso reaction blocks from Barnstead International, Dubuque, Iowa 52004-0797, USA or reaction stations from Radleys, Shirehill, Saffron Walden, Essex, CB11 3AZ, England or MultiPROBE automated workstations from Perkin Elmer, Waltham, Mass. 02451, USA. For the parallel purification of compounds of the formula (I) and salts thereof or of intermediates produced during the preparation, there are available, inter alia, chromatography apparatuses, for example from ISCO, Inc., 4700 Superior Street, Lincoln, Nebr. 68504, USA. 
     The apparatuses listed lead to a modular procedure in which the individual process steps are automated, but between the process steps manual operations have to be carried out. This can be circumvented by using partly or completely integrated automation systems in which the respective automation modules are operated, for example, by robots. Automation systems of this type can be acquired, for example, from Caliper, Hopkinton, Mass. 01748, USA. 
     The implementation of single or several synthesis steps can be supported through the use of polymer-supported reagents/scavenger resins. The specialist literature describes a series of experimental protocols, for example in ChemFiles, Vol. 4, No. 1, Polymer-Supported Scavengers and Reagents for Solution-Phase Synthesis (Sigma-Aldrich). 
     Besides the methods described here, the preparation of compounds of the formula (I) and salts thereof can take place completely or partially by solid-phase supported methods. For this purpose, individual intermediates or all intermediates in the synthesis or a synthesis adapted for the corresponding procedure are bonded to a synthesis resin. Solid-phase supported synthesis methods are sufficiently described in the specialist literature, e.g. Barry A. Bunin in “The Combinatorial Index”, Verlag Academic Press, 1998 and Combinatorial Chemistry—Synthesis, Analysis, Screening (editor Gunther Jung), Verlag Wiley, 1999. The use of solid-phase supported synthesis methods permits a series of protocols known in the literature, which again can be carried out manually or in an automated manner. The reactions can be carried out, for example, by means of IRORI technology in microreactors from Nexus Biosystems, 12140 Community Road, Poway, CA92064, USA. 
     Both on a solid phase and in liquid phase can the procedure of individual or several synthesis steps be supported through the use of microwave technology. The specialist literature describes a series of experimental protocols, for example in Microwaves in Organic and Medicinal Chemistry (editors C. O. Kappe and A. Stadler), Verlag Wiley, 2005. 
     The preparation according to the process described here produces compounds of the formula (I) and their salts in the form of substance collections which are called libraries. The present invention also provides libraries which comprise at least two compounds of the formula (I) and their salts. 
     The compounds of the formula (I) according to the invention (and/or their salts), hereinbelow also referred to together as “compounds according to the invention”, have excellent herbicidal efficacy against a broad spectrum of economically important monocotyledonous and dicotyledonous annual weed plants. The active compounds act efficiently even on perennial weeds which produce shoots from rhizomes, root stocks and other perennial organs and which are difficult to control. 
     The present invention therefore also relates to a method for controlling unwanted plants or for regulating the growth of plants, preferably in crops of plants, where one or more compound(s) according to the invention is/are applied to the plants (for example harmful plants such as monocotyledonous or dicotyledonous weeds or undesired crop plants), to the seeds (for example grains, seeds or vegetative propagules such as tubers or shoot parts with buds) or to the area on which the plants grow (for example the area under cultivation). In this context, the compounds according to the invention can be applied for example pre-sowing (if appropriate also by incorporation into the soil), pre-emergence or post-emergence. Specific examples may be mentioned of some representatives of the monocotyledonous and dicotyledonous weed flora which can be controlled by the compounds according to the invention, without the enumeration being restricted to certain species. 
     Monocotyledonous harmful plants of the genera:  Aegilops, Agropyron, Agrostis, Alopecurus, Apera, Avena, Brachiaria, Bromus, Cenchrus, Commelina, Cynodon, Cyperus, Dactyloctenium, Digitaria, Echinochloa, Eleocharis, Eleusine, Eragrostis, Eriochloa, Festuca, Fimbristylis, Heteranthera, Imperata, Ischaemum, Leptochloa, Lolium, Monochoria, Panicum, Paspalum, Phalaris, Phleum, Poa, Rottboellia, Sagittaria, Scirpus, Setaria, Sorghum.    
     Dicotyledonous broad-leaved weeds of the genera:  Abutilon, Amaranthus, Ambrosia, Anoda, Anthemis, Aphanes, Artemisia, Atriplex, Bellis, Bidens, Capsella, Carduus, Cassia, Centaurea, Chenopodium, Cirsium, Convolvulus, Datura, Desmodium, Emex, Erysimum, Euphorbia, Galeopsis, Galinsoga, Galium, Hibiscus, Ipomoea, Kochia, Lamium, Lepidium, Lindernia, Matricaria, Mentha, Mercurialis, Mullugo, Myosotis, Papaver, Pharbitis, Plantago, Polygonum, Portulaca, Ranunculus, Raphanus, Rorippa, Rotala, Rumex, Salsola, Senecio, Sesbania, Sida, Sinapis, Solanum, Sonchus, Sphenoclea, Stellaria, Taraxacum, Thlaspi, Trifolium, Urtica, Veronica, Viola, Xanthium.    
     If the compounds according to the invention are applied to the soil surface before germination, the weed seedlings are either prevented completely from emerging or else the weeds grow until they have reached the cotyledon stage, but then their growth stops, and, eventually, after three to four weeks have elapsed, they die completely. 
     If the active compounds are applied post-emergence to the green parts of the plants, growth stops after the treatment, and the harmful plants remain at the growth stage of the point of time of application, or they die completely after a certain time, so that in this manner competition by the weeds, which is harmful to the crop plants, is eliminated very early and in a sustained manner. 
     Although the compounds according to the invention display an outstanding herbicidal activity against monocotyledonous and dicotyledonous weeds, crop plants of economically important crops, for example dicotyledonous crops of the genera  Arachis, Beta, Brassica, Cucumis, Cucurbita, Helianthus, Daucus, Glycine, Gossypium, Ipomoea, Lactuca, Linum, Lycopersicon, Nicotiana, Phaseolus, Pisum, Solanum, Vicia , or monocotyledonous crops of the genera  Allium, Ananas, Asparagus, Avena, Hordeum, Oryza, Panicum, Saccharum, Secale, Sorghum, Triticale, Triticum, Zea , in particular  Zea  and  Triticum , are damaged only to an insignificant extent, or not at all, depending on the structure of the respective compound according to the invention and its application rate. This is why the present compounds are highly suitable for the selective control of unwanted plant growth in plant crops such as agriculturally useful plants or ornamentals. 
     Moreover, the compounds according to the invention (depending on their respective structure and the application rate applied) have outstanding growth-regulatory properties in crop plants. They engage in the plant&#39;s metabolism in a regulatory fashion and can therefore be employed for the influencing, in a targeted manner, of plant constituents and for facilitating harvesting, such as, for example, by triggering desiccation and stunted growth. Moreover, they are also suitable for generally controlling and inhibiting unwanted vegetative growth without destroying the plants in the process. Inhibiting the vegetative growth plays an important role in many monocotyledonous and dicotyledonous crops since for example lodging can be reduced, or prevented completely, hereby. 
     By virtue of their herbicidal and plant-growth-regulatory properties, the active compounds can also be employed for controlling harmful plants in crops of genetically modified plants which are known or which are yet to be developed. In general, the transgenic plants are distinguished by especially advantageous properties, for example by resistances to certain pesticides, mainly certain herbicides, resistances to plant diseases or causative organisms of plant diseases, such as certain insects or microorganisms such as fungi, bacteria or viruses. Other specific characteristics relate, for example, to the harvested material with regard to quantity, quality, storability, composition and specific constituents. Thus, transgenic plants are known whose starch content is increased, or whose starch quality is altered, or those where the harvested material has a different fatty acid composition. Further particular characteristics may lie in tolerance or resistance to abiotic stressors, for example, heat, cold, drought, salt, and ultraviolet radiation. 
     It is preferred to use the compounds of the formula (I) according to the invention or their salts in economically important transgenic crops of useful plants and ornamentals, for example of cereals such as wheat, barley, rye, oats, millet, rice, cassaya and corn or else crops of sugar beet, cotton, soybean, oilseed rape, potato, tomato, peas and other vegetables. 
     It is possible with preference to employ the compounds of the formula (I) as herbicides in crops of useful plants which are resistant, or have been made resistant by recombinant means, to the phytotoxic effects of the herbicides. 
     Conventional methods of generating novel plants which have modified properties in comparison to plants occurring to date consist, for example, in traditional breeding methods and the generation of mutants. Alternatively, novel plants with altered properties can be generated with the aid of recombinant methods (see, for example, EP 0221044, EP 0131624). For example, the following have been described in several cases:
         the modification, by recombinant technology, of crop plants with the aim of modifying the starch synthesized in the plants (for example WO 92/011376 A, WO 92/014827 A, WO 91/019806 A),   transgenic crop plants which are resistant to certain herbicides of the glufosinate type (cf., for example, EP-A-0242236, EP-A-0242246) or of the glyphosate type (WO 92/000377 A) or of the sulfonylurea type (EP-A-0257993, U.S. Pat. No. 5,013,659), or to combinations or mixtures of these herbicides which are resistant as a result of ‘gene stacking’, such as transgenic crop plants, e.g., corn or soybean, with the trade name or with the designation Optimum™ GAT™ (glyphosate ALS tolerant).   transgenic crop plants, for example cotton, with the capability of producing  Bacillus thuringiensis  toxins (Bt toxins), which make the plants resistant to certain pests (EP-A-0142924, EP-A-0193259),   transgenic crop plants with a modified fatty acid composition (WO 91/013972 A),   genetically modified crop plants with novel constituents or secondary metabolites, for example novel phytoalexins, which bring about an increased disease resistance (EPA 0309862, EPA0464461),   genetically modified plants with reduced photorespiration which feature higher yields and higher stress tolerance (EPA 0305398),   transgenic crop plants which produce pharmaceutically or diagnostically important proteins (“molecular pharming”),   transgenic crop plants which are distinguished by higher yields or better quality,   transgenic crop plants which are distinguished by a combination, for example, of the abovementioned novel properties (“gene stacking”).       

     A large number of molecular-biological techniques by means of which novel transgenic plants with modified properties can be generated are known in principle; see, for example, I. Potrykus and G. Spangenberg (eds.) Gene Transfer to Plants, Springer Lab Manual (1995), Springer Verlag Berlin, Heidelberg. or Christou, “Trends in Plant Science” 1 (1996) 423-431. 
     To carry out such recombinant manipulations, nucleic acid molecules which allow mutagenesis or sequence changes by recombination of DNA sequences can be introduced into plasmids. For example, base substitutions can be carried out, part-sequences can be removed, or natural or synthetic sequences may be added with the aid of standard methods. To link the DNA fragments with one another, it is possible to add adapters or linkers to the fragments; see, for example, Sambrook et al., 1989, Molecular Cloning, A Laboratory Manual, 2nd ed., Cold Spring Harbor Laboratory Press, Cold Spring Harbor, N.Y.; or Winnacker “Gene and Klone”, VCH Weinheim 2nd ed., 1996. 
     For example, the generation of plant cells with a reduced activity of a gene product can be achieved by expressing at least one corresponding antisense RNA, a sense RNA for achieving a cosuppression effect or by expressing at least one suitably constructed ribozyme which specifically cleaves transcripts of the abovementioned gene product. 
     To this end, it is possible to use DNA molecules which encompass the entire coding sequence of a gene product inclusive of any flanking sequences which may be present, and also DNA molecules which only encompass portions of the coding sequence, it being necessary for these portions to be long enough to have an antisense effect in the cells. The use of DNA sequences which have a high degree of homology to the coding sequences of a gene product, but are not completely identical to them, is also possible. 
     When expressing nucleic acid molecules in plants, the protein synthesized can be localized in any desired compartment of the plant cell. However, to achieve localization in a particular compartment, it is possible, for example, to link the coding region with DNA sequences which ensure localization in a particular compartment. Such sequences are known to those skilled in the art (see, for example, Braun et al., EMBO J. 11 (1992), 3219-3227; Wolter et al., Proc. Natl. Acad. Sci. USA 85 (1988), 846-850; Sonnewald et al., Plant J. 1 (1991), 95-106). The nucleic acid molecules can also be expressed in the organelles of the plant cells. 
     The transgenic plant cells can be regenerated by known techniques to give rise to entire plants. In principle, the transgenic plants can be plants of any desired plant species, i.e. not only monocotyledonous, but also dicotyledonous, plants. 
     Thus, transgenic plants can be obtained whose properties are altered by overexpression, suppression or inhibition of homologous (=natural) genes or gene sequences or the expression of heterologous (=foreign) genes or gene sequences. 
     It is preferred to employ the compounds (I) according to the invention in transgenic crops which are resistant to growth regulators such as, for example, 2,4 D dicamba, or to herbicides which inhibit essential plant enzymes, for example acetolactate synthases (ALS), EPSP synthases, glutamine synthases (GS) or hydroxyphenylpyruvate dioxygenases (HPPD), or to herbicides from the group of the sulfonylureas, the glyphosates, glufosinates or benzoylisoxazoles and analogous active compounds, or to any combinations of these active compounds. 
     With particular preference the compounds according to the invention can be used in transgenic crop plants which are resistant to a combination of glyphosates and glufosinates, glyphosates and sulfonylureas or imidazolinones. With very particular preference the compounds according to the invention can be used in transgenic crop plants such as, for example, corn or soybean with the tradename or the designation Optimum™ GAT™ (glyphosate ALS tolerant). 
     When the active compounds according to the invention are used in transgenic crops, effects are frequently observed—in addition to the effects on harmful plants which can be observed in other crops—which are specific for the application in the transgenic crop in question, for example a modified or specifically widened spectrum of weeds which can be controlled, modified application rates which may be employed for application, preferably good combinability with the herbicides to which the transgenic crop is resistant, and an effect on growth and yield of the transgenic crop plants. 
     The invention therefore also relates to the use of the compounds of the formula (I) according to the invention as herbicides for controlling harmful plants in transgenic crop plants. 
     The compounds according to the invention can be used in the form of wettable powders, emulsifiable concentrates, sprayable solutions, dusting products or granules in the customary formulations. The invention therefore also provides herbicidal and plant growth-regulating compositions which comprise the compounds according to the invention. 
     The compounds according to the invention can be formulated in various ways according to which biological and/or physicochemical parameters are mandated. Possible formulations include, for example: wettable powders (WP), water-soluble powders (SP), water-soluble concentrates, emulsifiable concentrates (EC), emulsions (EW) such as oil-in-water and water-in-oil emulsions, sprayable solutions, suspension concentrates (SC), oil- or water-based dispersions, oil-miscible solutions, capsule suspensions (CS), dusting products (DP), seed-dressing products, granules for scattering and soil application, granules (GR) in the form of microgranules, spray granules, coated granules and adsorption granules, water-dispersible granules (WG), water-soluble granules (SG), ULV formulations, microcapsules and waxes. These individual types of formulation are known in principle and are described, for example, in: Winnacker-Küchler, “Chemische Technologie” [Chemical technology], Volume 7, C. Hanser Verlag Munich, 4th Ed. 1986; Wade van Valkenburg, “Pesticide Formulations”, Marcel Dekker, N.Y., 1973; K. Martens, “Spray Drying” Handbook, 3rd Ed. 1979, G. Goodwin Ltd. London. 
     The necessary formulation assistants, such as inert materials, surfactants, solvents and further additives, are likewise known and are described, for example, in: Watkins, “Handbook of Insecticide Dust Diluents and Carriers”, 2nd Ed., Darland Books, Caldwell N.J.; H.v. Olphen, “Introduction to Clay Colloid Chemistry”; 2nd Ed., J. Wiley &amp; Sons, N.Y.; C. Marsden, “Solvents Guide”; 2nd Ed., Interscience, N.Y. 1963; McCutcheon&#39;s “Detergents and Emulsifiers Annual”, MC Publ. Corp., Ridgewood N.J.; Sisley and Wood, “Encyclopedia of Surface Active Agents”, Chem. Publ. Co. Inc., N.Y. 1964; Schonfeldt, “Grenzflächenaktive Äthylenoxidaddukte” [Interface-active ethylene oxide adducts], Wiss. Verlagsgesell., Stuttgart 1976; Winnacker-Küchler, “Chemische Technologie”, Volume 7, C. Hanser Verlag Munich, 4th Ed. 1986. 
     Based on these formulations, it is also possible to produce combinations with other pesticidally active compounds, such as, for example, insecticides, acaricides, herbicides, fungicides, and also with safeners, fertilizers and/or growth regulators, for example in the form of a finished formulation or as a tank mix. Suitable safeners are, for example, mefenpyr-diethyl, cyprosulfamide, isoxadifen-ethyl, cloquintocet-mexyl and dichlormid. 
     Wettable powders are preparations which can be dispersed uniformly in water and, as well as the active compound, apart from a diluent or inert substance, also comprise surfactants of the ionic and/or nonionic type (wetting agents, dispersants), for example polyoxyethylated alkylphenols, polyoxyethylated fatty alcohols, polyoxyethylated fatty amines, fatty alcohol polyglycol ether sulfates, alkanesulfonates, alkylbenzenesulfonates, sodium lignosulfonate, sodium 2,2′-dinaphthylmethane-6,6′-disulfonate, sodium dibutylnaphthalenesulfonate or else sodium oleoylmethyltaurinate. To prepare the wettable powders, the herbicidally active compounds are ground finely, for example in customary apparatus such as hammer mills, blower mills and air-jet mills, and simultaneously or subsequently mixed with the formulation assistants. 
     Emulsifiable concentrates are prepared by dissolving the active compound in an organic solvent, for example butanol, cyclohexanone, dimethylformamide, xylene or else relatively high-boiling aromatics or hydrocarbons or mixtures of the organic solvents with addition of one or more surfactants of the ionic and/or nonionic type (emulsifiers). The emulsifiers used may, for example, be: calcium alkylarylsulfonate salts such as calcium dodecylbenzenesulfonate, or nonionic emulsifiers such as fatty acid polyglycol esters, alkylaryl polyglycol ethers, fatty alcohol polyglycol ethers, propylene oxide-ethylene oxide condensation products, alkyl polyethers, sorbitan esters, for example sorbitan fatty acid esters, or polyoxyethylene sorbitan esters, for example polyoxyethylene sorbitan fatty acid esters. 
     Dusts are obtained by grinding the active compound with finely distributed solid substances, for example talc, natural clays, such as kaolin, bentonite and pyrophyllite, or diatomaceous earth. 
     Suspension concentrates may be water- or oil-based. They may be prepared, for example, by wet grinding by means of commercial bead mills and optional addition of surfactants as have, for example, already been listed above for the other formulation types. 
     Emulsions, for example oil-in-water emulsions (EW), can be prepared, for example, by means of stirrers, colloid mills and/or static mixers using aqueous organic solvents and optionally surfactants, as have, for example, already been listed above for the other formulation types. 
     Granules can be prepared either by spraying the active compound onto granular inert material capable of adsorption or by applying active compound concentrates to the surface of carrier substances, such as sand, kaolinites or granular inert material, by means of adhesives, for example polyvinyl alcohol, sodium polyacrylate or mineral oils. Suitable active compounds can also be granulated in the manner customary for the preparation of fertilizer granules—if desired as a mixture with fertilizers. 
     Water-dispersible granules are prepared generally by the customary processes such as spray-drying, fluidized bed granulation, pan granulation, mixing with high-speed mixers and extrusion without solid inert material. 
     For the preparation of pan, fluidized bed, extruder and spray granules, see, for example, processes in “Spray-Drying Handbook” 3rd ed. 1979, G. Goodwin Ltd., London; J. E. Browning, “Agglomeration”, Chemical and Engineering 1967, pages 147 ff; “Perry&#39;s Chemical Engineer&#39;s Handbook”, 5th Ed McGraw-Hill, New York 1973, p. 8-57. 
     For further details regarding the formulation of crop protection compositions, see, for example, G. C. Klingman, “Weed Control as a Science”, John Wiley and Sons, Inc., New York, 1961, pages 81-96 and J. D. Freyer, S. A. Evans, “Weed Control Handbook”, 5th Ed., Blackwell Scientific Publications, Oxford, 1968, pages 101-103. 
     The agrochemical formulations contain generally from 0.1 to 99% by weight, in particular from 0.1 to 95% by weight, of compounds according to the invention. 
     In wettable powders, the active compound concentration is, for example, from about 10 to 90% by weight, the remainder to 100% by weight consisting of customary formulation components. In the case of emulsifiable concentrates, the active compound concentration can be from about 1 to 90, preferably from 5 to 80, % by weight. Formulations in the form of dusts comprise from 1 to 30% by weight of active compound, preferably usually from 5 to 20% by weight of active compound; sprayable solutions contain from about 0.05 to 80% by weight, preferably from 2 to 50% by weight of active compound. In the case of water-dispersible granules, the active compound content depends partially on whether the active compound is present in liquid or solid form and on which granulation auxiliaries, fillers, etc., are used. In the water-dispersible granules, the content of active compound is, for example, between 1 and 95% by weight, preferably between 10 and 80% by weight. 
     In addition, the active compound formulations mentioned optionally comprise the respective customary adhesives, wetting agents, dispersants, emulsifiers, penetrants, preservatives, antifreeze agents and solvents, fillers, carriers and dyes, defoamers, evaporation inhibitors and agents which influence the pH and the viscosity. 
     Based on these formulations, it is also possible to produce combinations with other pesticidally active compounds, such as, for example, insecticides, acaricides, herbicides, fungicides, and also with safeners, fertilizers and/or growth regulators, for example in the form of a finished formulation or as a tank mix. 
     Active compounds which can be employed in combination with the compounds according to the invention in mixed formulations or in the tank mix are, for example, known active compounds which are based on the inhibition of, for example, acetolactate synthase, acetyl-CoA carboxylase, cellulose synthase, enolpyruvylshikimate-3-phosphate synthase, glutamine synthetase, p-hydroxyphenylpyruvate dioxygenase, phytoen desaturase, photosystem I, photosystem II, protoporphyrinogen oxidase, as are described in, for example, Weed Research 26 (1986) 441-445 or “The Pesticide Manual”, 15th edition, The British Crop Protection Council and the Royal Soc. of Chemistry, 2003 and the literature cited therein. Known herbicides or plant growth regulators which can be combined with the compounds according to the invention are, for example, the following active compounds (the compounds are either designated by the common name according to the International Organization for Standardization (ISO) or by the chemical name, or by the code number) and always comprise all use forms such as acids, salts, esters and isomers such as stereoisomers and optical isomers. Here, by way of example, one and in some cases a plurality of use forms are mentioned: acetochlor, acibenzolar, acibenzolar-S-methyl, acifluorfen, acifluorfen-sodium, aclonifen, alachlor, allidochlor, alloxydim, alloxydim-sodium, ametryn, amicarbazone, amidochlor, amidosulfuron, aminocyclopyrachlor, aminopyralid, amitrole, ammonium sulfamate, ancymidol, anilofos, asulam, atrazine, azafenidin, azimsulfuron, aziprotryn, beflubutamid, benazolin, benazolin-ethyl, bencarbazone, benfluralin, benfuresate, bensulide, bensulfuron, bensulfuron-methyl, bentazone, benzfendizone, benzobicyclon, benzofenap, benzofluor, benzoylprop, bicyclopyrone, bifenox, bilanafos, bilanafos-sodium, bispyribac, bispyribac-sodium, bromacil, bromobutide, bromofenoxim, bromoxynil, bromuron, buminafos, busoxinone, butachlor, butafenacil, butamifos, butenachlor, butralin, butroxydim, butylate, cafenstrole, carbetamide, carfentrazone, carfentrazone-ethyl, chlomethoxyfen, chloramben, chlorazifop, chlorazifop-butyl, chlorbromuron, chlorbufam, chlorfenac, chlorfenac-sodium, chlorfenprop, chlorflurenol, chlorflurenol-methyl, chloridazon, chlorimuron, chlorimuron-ethyl, chlormequat chloride, chlornitrofen, chlorophthalim, chlorthal-dimethyl, chlorotoluron, chlorsulfuron, cinidon, cinidon-ethyl, cinmethylin, cinosulfuron, clethodim, clodinafop, clodinafop-propargyl, clofencet, clomazone, clomeprop, cloprop, clopyralid, cloransulam, cloransulam-methyl, cumyluron, cyanamide, cyanazine, cyclanilide, cycloate, cyclosulfamuron, cycloxydim, cycluron, cyhalofop, cyhalofop-butyl, cyperquat, cyprazine, cyprazole, 2,4-D, 2,4-DB, daimuron/dymron, dalapon, daminozide, dazomet, n-decanol, desmedipham, desmetryn, detosyl pyrazolate (DTP), diallate, dicamba, dichlobenil, dichlorprop, dichlorprop-P, diclofop, diclofop-methyl, diclofop-P-methyl, diclosulam, diethatyl, diethatyl-ethyl, difenoxuron, difenzoquat, diflufenican, diflufenzopyr, diflufenzopyr-sodium, dimefuron, dikegulac-sodium, dimefuron, dimepiperate, dimethachlor, dimethametryn, dimethenamid, dimethenamid-P, dimethipin, dimetrasulfuron, dinitramine, dinoseb, dinoterb, diphenamid, dipropetryn, diquat, diquat dibromide, dithiopyr, diuron, DNOC, eglinazine-ethyl, endothal, EPTC, esprocarb, ethalfluralin, ethametsulfuron, ethametsulfuron-methyl, ethephon, ethidimuron, ethiozin, ethofumesate, ethoxyfen, ethoxyfen-ethyl, ethoxysulfuron, etobenzanid, F-5331, i.e. N-[2-chloro-4-fluoro-5-[4-(3-fluoropropyl)-4,5-dihydro-5-oxo-1H-tetrazol-1-yl]-phenyl]-ethanesulfonamide, F-7967, i.e., 3-[7-chloro-5-fluoro-2-(trifluoromethyl)-1H-benzimidazol-4-yl]-1-methyl-6-(trifluoromethyl)pyrimidine-2,4(1H, 3H)-dione, fenoprop, fenoxaprop, fenoxaprop-P, fenoxaprop-ethyl, fenoxaprop-P-ethyl, fenoxasulfone, fentrazamide, fenuron, flamprop, flamprop-M-isopropyl, flamprop-M-methyl, flazasulfuron, florasulam, fluazifop, fluazifop-P, fluazifop-butyl, fluazifop-P-butyl, fluazolate, flucarbazone, flucarbazone-sodium, flucetosulfuron, fluchloralin, flufenacet (thiafluamide), flufenpyr, flufenpyr-ethyl, flumetralin, flumetsulam, flumiclorac, flumiclorac-pentyl, flumioxazin, flumipropyn, fluometuron, fluorodifen, fluoroglycofen, fluoroglycofen-ethyl, flupoxam, flupropacil, flupropanate, flupyrsulfuron, flupyrsulfuron-methyl-sodium, flurenol, flurenol-butyl, fluridone, fluorochloridone, fluoroxypyr, fluoroxypyr-meptyl, flurprimidol, flurtamone, fluthiacet, fluthiacet-methyl, fluthiamide, fomesafen, foramsulfuron, forchlorfenuron, fosamine, furyloxyfen, gibberellic acid, glufosinate, glufosinate-ammonium, glufosinate-P, glufosinate-P-ammonium, glufosinate-P-sodium, glyphosate, glyphosate-isopropylammonium, H-9201, i.e., O-(2,4-dimethyl-6-nitrophenyl)-O-ethyl-isopropylphosphoramidothioate, halosafen, halosulfuron, halosulfuron-methyl, haloxyfop, haloxyfop-P, haloxyfop-ethoxyethyl, haloxyfop-P-ethoxyethyl, haloxyfop-methyl, haloxyfop-P-methyl, hexazinone, HW-02, i.e., 1-(dimethoxyphosphoryl)-ethyl(2,4-dichlorophenoxy)acetate, imazamethabenz, imazamethabenz-methyl, imazamox, imazamox-ammonium, imazapic, imazapyr, imazapyr-isopropylammonium, imazaquin, imazaquin-ammonium, imazethapyr, imazethapyr-ammonium, imazosulfuron, inabenfide, indanofan, indaziflam, indoleacetic acid (IAA), 4-indol-3-ylbutyric acid (IBA), iodosulfuron, iodosulfuron-methyl-sodium, ioxynil, ipfencarbazone, isocarbamid, isopropalin, isoproturon, isouron, isoxaben, isoxachlortole, isoxaflutole, isoxapyrifop, KUH-043, i.e., 3-({[5-(difluoromethyl)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}sulfonyl)-5,5-dimethyl-4,5-dihydro-1,2-oxazole, karbutilate, ketospiradox, lactofen, lenacil, linuron, maleic hydrazide, MCPA, MCPB, MCPB-methyl, -ethyl and -sodium, mecoprop, mecoprop-sodium, mecoprop-butotyl, mecoprop-P-butotyl, mecoprop-P-dimethylammonium, mecoprop-P-2-ethylhexyl, mecoprop-P-potassium, mefenacet, mefluidide, mepiquat-chloride, mesosulfuron, mesosulfuron-methyl, mesotrione, methabenzthiazuron, metam, metamifop, metamitron, metazachlor, metazasulfuron, methazole, methiopyrsulfuron, methiozolin, methoxyphenone, methyldymron, 1-methylcyclopropene, methylisothiocyanate, metobenzuron, metobromuron, metolachlor, S-metolachlor, metosulam, metoxuron, metribuzin, metsulfuron, metsulfuron-methyl, molinate, monalide, monocarbamide, monocarbamide dihydrogensulfate, monolinuron, monosulfuron, monosulfuron-ester, monuron, MT 128, i.e., 6-chloro-N-[(2E)-3-chloroprop-2-en-1-yl]-5-methyl-N-phenylpyridazin-3-amine, MT-5950, i.e. N-[3-chloro-4-(1-methylethyl)-phenyl]-2-methylpentanamide, NGGC-011, naproanilide, napropamide, naptalam, NC-310, i.e. 4-(2,4-dichlorobenzoyl)-1-methyl-5-benzyloxypyrazole, neburon, nicosulfuron, nipyraclofen, nitralin, nitrofen, nitrophenolate sodium (isomer mixture), nitrofluorfen, nonanoic acid, norflurazon, orbencarb, orthosulfamuron, oryzalin, oxadiargyl, oxadiazon, oxasulfuron, oxaziclomefone, oxyfluorfen, paclobutrazol, paraquat, paraquat-dichlorid, pelargonic acid (nonanoic acid), pendimethalin, pendralin, penoxsulam, pentanochlor, pentoxazone, perfluidone, pethoxamid, phenisopham, phenmedipham, phenmedipham-ethyl, picloram, picolinafen, pinoxaden, piperophos, pirifenop, pirifenop-butyl, pretilachlor, primisulfuron, primisulfuron-methyl, probenazole, profluazol, procyazine, prodiamine, prifluraline, profoxydim, prohexadione, prohexadione-calcium, prohydrojasmone, prometon, prometryn, propachlor, propanil, propaquizafop, propazine, propham, propisochlor, propoxycarbazone, propoxycarbazone-sodium, propyrisulfuron, propyzamide, prosulfalin, prosulfocarb, prosulfuron, prynachlor, pyraclonil, pyraflufen, pyraflufen-ethyl, pyrasulfotole, pyrazolynate (pyrazolate), pyrazosulfuron, pyrazosulfuron-ethyl, pyrazoxyfen, pyribambenz, pyribambenz-isopropyl, pyribambenz-propyl, pyribenzoxim, pyributicarb, pyridafol, pyridate, pyriftalid, pyriminobac, pyriminobac-methyl, pyrimisulfan, pyrithiobac, pyrithiobac-sodium, pyroxasulfone, pyroxsulam, quinclorac, quinmerac, quinoclamine, quizalofop, quizalofop-ethyl, quizalofop-P, quizalofop-P-ethyl, quizalofop-P-tefuryl, rimsulfuron, saflufenacil, secbumeton, sethoxydim, siduron, simazine, simetryn, SN-106279, i.e. methyl-(2R)-2({7-[2-chloro-4-(trifluoromethyl)phenoxy]-2-naphthyl}oxy)propanoate, sulcotrione, sulfallate (CDEC), sulfentrazone, sulfometuron, sulfometuron-methyl, sulfosate (glyphosate-trimesium), sulfosulfuron, SYN-523, SYP-249, i.e., 1-ethoxy-3-methyl-1-oxobut-3-en-2-yl-5-[2-chloro-4-(trifluoromethyl)phenoxy]-2-nitrobenzoate, SYP-300, i.e., 1-[7-fluoro-3-oxo-4-(prop-2-yn-1-yl)-3,4-dihydro-2H-1,4-benzoxazin-6-yl]-3-propyl-2-thioxoimidazolidine-4,5-dione, tebutam, tebuthiuron, tecnazene, tefuryltrione, tembotrione, tepraloxydim, terbacil, terbucarb, terbuchlor, terbumeton, terbuthylazine, terbutryn, thenylchlor, thiafluamide, thiazafluoron, thiazopyr, thidiazimin, thidiazuron, thiencarbazone, thiencarbazone-methyl, thifensulfuron, thifensulfuron-methyl, thiobencarb, tiocarbazil, topramezone, tralkoxydim, triallate, triasulfuron, triaziflam, triazofenamide, tribenuron, tribenuron-methyl, trichloroacetic acid (TCA), triclopyr, tridiphane, trietazine, trifloxysulfuron, trifloxysulfuron-sodium, trifluralin, triflusulfuron, triflusulfuron-methyl, trimeturon, trinexapac, trinexapac-ethyl, tritosulfuron, tsitodef, uniconazole, uniconazole-P, vernolate, ZJ-0862 i.e. 3,4-dichloro-N-{2-[(4,6-dimethoxypyrimidin-2-yl)oxy]benzyl}aniline, and also the following compounds: 
     
       
         
         
             
             
         
       
     
     For application, the formulations present in commercial form are, if appropriate, diluted in a customary manner, for example, in the case of wettable powders, emulsifiable concentrates, dispersions and water-dispersible granules, with water. Preparations in the form of dusts, granules for soil application or granules for broadcasting and sprayable solutions are usually not diluted further with other inert substances prior to application. 
     The required application rate of the compounds of the formula (I) varies according to the external conditions such as, inter alia, temperature, humidity and the type of herbicide used. It may vary within wide limits, for example between 0.001 and 1.0 kg/ha or more of active substance; however, preferably it is between 0.005 and 750 g/ha. 
     The examples which follow illustrate the invention. 
     A. Chemical Examples 
     Preparation of 5-hydroxy-1,3-dimethyl-4-(2-methyl-3-methylthio-4-pentafluoroethyl-benzoyl)pyrazole (tabular example No. 3-145) 
     Step 1: Synthesis of 3-fluoro-4-(pentafluoroethyl)bromobenzene 
     13.2 g (91.9 mmol) of copper(I) bromide were cooled to −5° C. in 80 ml of dry N,N-dimethylformamide. Under nitrogen, 14.7 g (76.7 mmol) of trimethyl-(pentafluoroethyl)silane were added. 4.45 g (76.7 mmol) of potassium fluoride (spray-dried) were added in portions over the course of 30 minutes at a rate such that the internal temperature remained below 0° C. The mixture was stirred at 0° C. for 1 hour and was then warmed to 20° C. over the course of 12 hours. Thereafter 10 ml of dry 1,3-dimethyl-2-imidazolidinone and 22 g (73.1 mmol) of 3-fluoro-4-iodo-bromobenzene were added. The contents were stirred at 75° C. for 14 hours. Then all of the volatile constituents were distilled off to dryness, the distillate being collected in a cold trap cooled with liquid nitrogen. The distillate was subsequently warmed to 20° C. and dissolved in 500 ml of diethyl ether. This solution was washed with four times 100 ml of water and then with two times 100 ml of saturated aqueous NaCl solution. The organic phase was then dried, and the solvent was removed on a Vigreux column. Subsequent distillation of the residue on a Vigreux column gave 16.1 g of product (boiling point: 86-87° C. (75 mmHg)) with a purity of 99% by weight. 
     Step 2: Synthesis of 3-fluoro-4-(pentafluoroethyl)benzoic acid 
     A solution of 16.0 g (99% by weight; 54.1 mmol) of 3-fluoro-4-(pentafluoroethyl)-bromobenzene in 110 ml of THF was cooled to −10° C. Added dropwise over the course of 30 minutes were 36.8 ml of a 2M (73.6 mmol) solution of isopropyl-magnesium chloride. The mixture was stirred at −10° C. for 2.5 hours and then cautiously poured onto an excess of dry ice. For working up, 130 ml of water were added, and the mixture was subsequently extracted once with 10 ml of diethyl ether. The aqueous phase was acidified with half-concentrated hydrochloric acid and then extracted with four times 150 ml of diethyl ether. The combined organic phases were dried and the filtrate was freed from the solvent. The residue was recrystallized from CHCl 3 , giving 10.7 g of product with a purity of 98% by weight. 
     Step 3: Synthesis of 3-fluor-2-methyl-4-(pentafluoroethyl)benzoic acid 
     5.00 g (98% by weight; 19.0 mmol) of 3-fluoro-4-(pentafluoroethyl)benzoic acid were introduced into 40 ml of dry tetrahydrofuran. 4.73 g (40.7 mmol) of 1,2-bis-(dimethylamino)ethane were added, and the mixture was then cooled to −40° C. Then 16.3 ml of a 2.5 M solution (40.7 mmol) of n-butyllithium in hexane were added dropwise at a rate such that the temperature was in a range from −33° C. to −35° C. The contents were stirred at −35° C. for 4 hours. Then a solution of 8.25 g (58.1 mmol) of iodomethane in 10 ml of dry THF was added dropwise, and the mixture was stirred at −35° C. for 1 hour. Thereafter the contents were warmed to room temperature (RT) and stirred at this temperature for 16 hours. For working up, 50 ml of 2M hydrochloric acid were cautiously added, and then the aqueous phase was extracted with diethyl ether. The combined organic phases were dried and freed from the solvents. The residue was stirred in n-heptane and subsequently filtered. This gave 2.33 g of residue as a clean product. The filtrate was freed from the solvent, and the residue was again stirred in n-heptane. Filtration produced 590 mg of residue, which was identified as a product with a purity of 70% by weight. 
     Step 4: Synthesis of methyl 3-fluoro-2-methyl-4-(pentafluoroethyl)benzoate 
     2.33 g (8.56 mmol) of 3-fluoro-2-methyl-4-(pentafluoroethyl)benzoic acid were introduced into 30 ml of methanol and admixed with 2 ml of concentrated sulfuric acid. The mixture was subsequently heated at reflux until a check by HPLC indicated full conversion. The contents were freed from the solvent, and the residue was taken up in water. The mixture was extracted twice with ethyl acetate, and the combined organic phases were washed once with saturated aqueous sodium hydrogen-carbonate solution. The organic phase was dried and freed from the solvent. The residue obtained was 2.1 g of clean product. 
     Step 5: Synthesis of methyl 2-methyl-3-(methylthio)-4-(pentafluoroethyl)benzoate 
     2.1 g (7.34 mmol) of methyl 3-fluoro-2-methyl-4-(pentafluoroethyl)benzoate were introduced into 20 ml of N,N-dimethylformamide and then admixed with 758 mg (95% by weight; 10.3 mmol) of sodium thiomethoxide. The mixture was stirred at RT for 2 hours and then freed from the solvent. The residue was taken up in ethyl acetate and water, the aqueous phase was extracted twice with ethyl acetate, and, finally, the combined organic phases were dried and freed from the solvent. The residue was purified by chromatography, giving 1.28 g of clean product. 
     Step 6: Synthesis of 2-methyl-3-(methylthio)-4-(pentafluoroethyl)benzoic acid 
     (No. 5-145) 
     530 mg (1.69 mmol) of methyl 2-methyl-3-(methylthio)-4-(pentafluoroethyl)benzoate were introduced into 10 ml of methanol and admixed with 0.5 ml of 20% strength aqueous sodium hydroxide solution. The contents were stirred at room temperature until a check on the reaction by thin-layer chromatography indicated complete conversion. The mixture was freed from the solvent, and the residue was taken up in a little water. The mixture was acidified with 1M hydrochloric acid, then stirred for 5 minutes and finally filtered. The residue obtained was 470 mg of clean product. 
     Step 7: Synthesis of 1,3-dimethyl-5-(2″-methyl-3″-(methylthio)-4″-(pentafluoroethyl)benzoyloxy)pyrazole 
     360 mg (1.20 mmol) of 2-methyl-3-(methylthio)-4-(pentafluoroethyl)benzoic acid were introduced into 20 ml of dry dichloromethane and admixed in succession with 198 mg (1.56 mmol) of oxalyl dichloride and also with two drops of N,N-dimethyl-formamide. After the end of evolution of gas, the mixture was heated under reflux for 10 minutes. When a check on the reaction by thin-layer chromatography had indicated complete conversion, the contents were freed from the solvent, and the residue was then taken up in 20 ml of dry dichloromethane. The mixture was admixed with 161 mg (1.44 mmol) of 5-hydroxy-1,3-dimethylpyrazole, and then 243 mg (2.40 mmol) of triethylamine were added dropwise. The contents were stirred at RT for 16 hours. For working up, 3 ml of 1M hydrochloric acid were added, and, following phase separation, the organic phase was freed from the solvent. The residue, finally, was purified by chromatography, giving 410 mg of clean product. 
     Step 8: Synthesis of 5-hydroxy-1,3-dimethyl-4-(2′-methyl-3′-(methylthio)-4′-(pentafluoroethyl)benzoyl)pyrazole (No. 3-145) 
     136 mg (0.345 mmol) of 1,3-dimethyl-5-(2′-methyl-3′-(methylthio)-4′-(pentafluoro-ethyl)benzoyloxy)pyrazole were introduced into 15 ml of acetonitrile and admixed in succession with 70 mg (0.69 mmol) of triethylamine and also with eight drops of trimethylsilyl cyanide. The mixture was stirred at RT for 16 hours. For working up, the contents were freed from the solvent, and the residue was taken up in 15 ml of dichloromethane. 3 ml of 1M hydrochloric acid were added, and, following phase separation, the organic phase was freed from the solvent. The residue was purified by chromatography, giving 71.3 mg of product with a purity of 95% by weight. 
     The examples listed in tables below were prepared in analogy to methods identified above or are obtainable in analogy to methods identified above. These compounds are very particularly preferred. 
     The abbreviations used have the following meanings: 
     
       
         
           
               
               
               
               
               
             
               
                   
                   
               
             
            
               
                   
                 Bu = butyl 
                 Et = ethyl 
                 Me = methyl 
                 Pr = propyl 
               
               
                   
                 i = iso 
                 s = secondary 
                 t = tertiary 
                 Ph = phenyl 
               
               
                   
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 1 
               
             
            
               
                   
               
               
                 Inventive compounds of the formula (I) in which R 2  is methyl, 
               
               
                 and R 3  and R 4  are each hydrogen 
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
            
           
           
               
               
               
               
               
               
            
               
                 No.  
                 X 
                 R 1   
                 n 
                 Y 
                 Physical data:  1 H-NMR: δ [CDCl 3 ] 
               
               
                   
               
               
                 1-1 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-2 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-3 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-4 
                 Me 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-5 
                 Me 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-6 
                 Me 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-7 
                 Me 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-8 
                 Me 
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-9 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-10 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-11 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-12 
                 Me 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-13 
                 Me 
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-14 
                 Me 
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-15 
                 Me 
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-16 
                 Me 
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-17 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-18 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-19 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-20 
                 Me 
                 i-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-21 
                 Me 
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-22 
                 Me 
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-23 
                 Me 
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-24 
                 Me 
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-25 
                 Et 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-26 
                 Et 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-27 
                 Et 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-28 
                 Et 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-29 
                 Et 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-30 
                 Et 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-31 
                 Et 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-32 
                 Et 
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 1-33 
                 Et 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-34 
                 Et 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-35 
                 Et 
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-36 
                 Et 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-37 
                 Et 
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-38 
                 Et 
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-39 
                 Et 
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-40 
                 Et 
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 1-41 
                 Et 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-42 
                 Et 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-43 
                 Et 
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-44 
                 Et 
                 i-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-45 
                 Et 
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-46 
                 Et 
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-47 
                 Et 
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-48 
                 Et 
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 1-49 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 1-50 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 1-51 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 1-52 
                 Me 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 1-53 
                 Me 
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-54 
                 Me  
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-55 
                 Me 
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-56 
                 Me 
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-57 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 1-58 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 1-59 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 1-60 
                 Me 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 1-61 
                 Me 
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-62 
                 Me 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-63 
                 Me 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-64 
                 Me 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-65 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 1-66 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 1-67 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 1-68 
                 Me 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 1-69 
                 Me 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-70 
                 Me 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-71 
                 Me 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-72 
                 Me 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-73 
                 Et 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 1-74 
                 Et 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 1-75 
                 Et 
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 1-76 
                 Et 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 1-77 
                 Et 
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-78 
                 Et 
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-79 
                 Et 
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-80 
                 Et 
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 1-81 
                 Et 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 1-82 
                 Et 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 1-83 
                 Et 
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 1-84 
                 Et 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 1-85 
                 Et 
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-86 
                 Et 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-87 
                 Et 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-88 
                 Et 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 1-89 
                 Et 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 1-90 
                 Et 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 1-91 
                 Et 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 1-92 
                 Et 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 1-93 
                 Et 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-94 
                 Et 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-95 
                 Et 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-96 
                 Et 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 1-97 
                 Me 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 1-98 
                 Me 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 1-99 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 1-100 
                 Me 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 1-101 
                 Me 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-102 
                 Me 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-103 
                 Me 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-104 
                 Me 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-105 
                 Me 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 1-106 
                 Me 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 1-107 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 1-108 
                 Me 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 1-109 
                 Me 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-110 
                 Me 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-111 
                 Me 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-112 
                 Me 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-113 
                 Me 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 1-114 
                 Me 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 1-115 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 1-116 
                 Me 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 1-117 
                 Me 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-118 
                 Me 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-119 
                 Me 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-120 
                 Me 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-121 
                 Et 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 1-122 
                 Et 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 1-123 
                 Et 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 1-124 
                 Et 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 1-125 
                 Et 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-126 
                 Et 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-127 
                 Et 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-128 
                 Et 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 1-129 
                 Et 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 1-130 
                 Et 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 1-131 
                 Et 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 1-132 
                 Et 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 1-133 
                 Et 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-134 
                 Et 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-135 
                 Et 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-136 
                 Et 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 1-137 
                 Et 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 1-138 
                 Et 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 1-139 
                 Et 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 1-140 
                 Et 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 1-141 
                 Et 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-142 
                 Et 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-143 
                 Et 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-144 
                 Et 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 1-145 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 7.61 (d, 1H), 7.47 (d, 1H), 
               
               
                   
                   
                   
                   
                   
                 7.31 (s, 1H), 3.72 (s, 3H), 
               
               
                   
                   
                   
                   
                   
                 2.69 (s, 3H), 2.30 (s, 3H) 
               
               
                 1-146 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 1-147 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 1-148 
                 Me 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 1-149 
                 Me 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-150 
                 Me 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-151 
                 Me 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-152 
                 Me 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-153 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 7.63 (d, 1H), 7.57 (d, 1H), 
               
               
                   
                   
                   
                   
                   
                 7.33 (s, 1H), 3.73 (s, 3H), 
               
               
                   
                   
                   
                   
                   
                 3.07 (s, 3H), 2.91 (s, 3H) 
               
               
                 1-154 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 1-155 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 1-156 
                 Me 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 1-157 
                 Me 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-158 
                 Me 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-159 
                 Me 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-160 
                 Me 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-161 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 7.76 (d, 1H), 7.64 (d, 1H), 
               
               
                   
                   
                   
                   
                   
                 7.30 (s, 1H), 3.73 (s, 3H), 
               
               
                   
                   
                   
                   
                   
                 3.29 (s, 3H), 2.77 (s, 3H) 
               
               
                 1-162 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 1-163 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 1-164 
                 Me 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 1-165 
                 Me 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-166 
                 Me 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-167 
                 Me 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-168 
                 Me 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-169 
                 Et 
                 Me 
                 0 
                 C 2 F 5   
                   
               
               
                 1-170 
                 Et 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 1-171 
                 Et 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 1-172 
                 Et 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 1-173 
                 Et 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-174 
                 Et 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-175 
                 Et 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-176 
                 Et 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 1-177 
                 Et 
                 Me 
                 1 
                 C 2 F 5   
                   
               
               
                 1-178 
                 Et 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 1-179 
                 Et 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 1-180 
                 Et 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 1-181 
                 Et 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-182 
                 Et 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-183 
                 Et 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-184 
                 Et 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 1-185 
                 Et 
                 Me 
                 2 
                 C 2 F 5   
                   
               
               
                 1-186 
                 Et 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 1-187 
                 Et 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 1-188 
                 Et 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 1-189 
                 Et 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-190 
                 Et 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-191 
                 Et 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-192 
                 Et 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 1-193 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-194 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-195 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-196 
                 Me 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-197 
                 Me 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-198 
                 Me 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-199 
                 Me 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-200 
                 Me 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-201 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-202 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-203 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-204 
                 Me 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-205 
                 Me 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-206 
                 Me 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-207 
                 Me 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-208 
                 Me 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-209 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-210 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-211 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-212 
                 Me 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-213 
                 Me 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-214 
                 Me 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-215 
                 Me 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-216 
                 Me 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-217 
                 Et 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-218 
                 Et 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-219 
                 Et 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-220 
                 Et 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-221 
                 Et 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-222 
                 Et 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-223 
                 Et 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-224 
                 Et 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 1-225 
                 Et 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-226 
                 Et 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-227 
                 Et 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-228 
                 Et 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-229 
                 Et 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-230 
                 Et 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-231 
                 Et 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-232 
                 Et 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 1-233 
                 Et 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-234 
                 Et 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-235 
                 Et 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-236 
                 Et 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-237 
                 Et 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-238 
                 Et 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-239 
                 Et 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-240 
                 Et 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 1-241 
                 Me 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 1-242 
                 Me 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 1-243 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 1-244 
                 Me 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 1-245 
                 Me 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-246 
                 Me 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-247 
                 Me 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-248 
                 Me 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-249 
                 Me 
                 Me  
                 1 
                 CHF 2   
                   
               
               
                 1-250 
                 Me 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 1-251 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 1-252 
                 Me 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 1-253 
                 Me 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-254 
                 Me 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-255 
                 Me 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-256 
                 Me 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-257 
                 Me 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 1-258 
                 Me 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 1-259 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 1-260 
                 Me 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 1-261 
                 Me 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 1-262 
                 Me 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 1-263 
                 Me 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 1-264 
                 Me 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-265 
                 Et 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 1-266 
                 Et 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 1-267 
                 Et 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 1-268 
                 Et 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 1-269 
                 Et 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-270 
                 Et 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-271 
                 Et 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-272 
                 Et 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 1-273 
                 Et 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 1-274 
                 Et 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 1-755 
                 Et 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 1-276 
                 Et 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 1-277 
                 Et 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-278 
                 Et 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-279 
                 Et 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-280 
                 Et 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 1-281 
                 Et 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 1-282 
                 Et 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 1-283 
                 Et 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 1-284 
                 Et 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 1-285 
                 Et 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 1-286 
                 Et 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 1-287 
                 Et 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 1-288 
                 Et 
                 t-Bu 
                 2 
                 CHF 2   
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 2 
               
             
            
               
                   
               
               
                 Inventive compounds of the formula (I) in which R 2  is ethyl,  
               
               
                 and R 3  and R 4  are each hydrogen 
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
            
           
           
               
               
               
               
               
               
            
               
                   
                   
                   
                   
                   
                 Physical data: 
               
               
                 No. 
                 X 
                 R 1   
                 n 
                 Y 
                   1 H-NMR: δ [CDCl 3 ] 
               
               
                   
               
               
                 2-1 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-2 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-3 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-4 
                 Me 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-5 
                 Me 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-6 
                 Me 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-7 
                 Me 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-8 
                 Me 
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-9 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-10 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-11 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-12 
                 Me 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-13 
                 Me 
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-14 
                 Me 
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-15 
                 Me 
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-16 
                 Me 
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-17 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-18 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-19 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-20 
                 Me 
                 i-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-21 
                 Me 
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-22 
                 Me 
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-23 
                 Me 
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-24 
                 Me 
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-25 
                 Et 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-26 
                 Et 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-27 
                 Et 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-28 
                 Et 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-29 
                 Et 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-30  
                 Et 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-31  
                 Et 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-32  
                 Et  
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 2-33  
                 Et 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-34 
                 Et 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-35  
                 Et  
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-36  
                 Et 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-37  
                 Et  
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-38  
                 Et  
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-39  
                 Et  
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-40  
                 Et  
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 2-41  
                 Et 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-42  
                 Et 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-43  
                 Et  
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-44  
                 Et 
                 i-Pr  
                 2 
                 CF 2 Cl 
                   
               
               
                 2-45  
                 Et  
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-46  
                 Et  
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-47  
                 Et  
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-48  
                 Et  
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 2-49 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 2-50  
                 Me 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 2-51  
                 Me  
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 2-52  
                 Me 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 2-53  
                 Me  
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-54  
                 Me  
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-55  
                 Me  
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-56  
                 Me  
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-57  
                 Me 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 2-58  
                 Me 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 2-59  
                 Me  
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 2-60  
                 Me 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 2-61  
                 Me  
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-62  
                 Me 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-63  
                 Me 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-64  
                 Me 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-65  
                 Me 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 2-66 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 2-67 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 2-68 
                 Me 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 2-69 
                 Me 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-70 
                 Me 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-71  
                 Me 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-72 
                 Me 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-73  
                 Et 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 2-74  
                 Et 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 2-75  
                 Et 
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 2-76  
                 Et 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 2-77  
                 Et 
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-78  
                 Et 
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-79  
                 Et 
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-80  
                 Et 
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 2-81  
                 Et 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 2-82  
                 Et 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 2-83  
                 Et 
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 2-84  
                 Et 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 2-85  
                 Et 
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-86  
                 Et 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-87  
                 Et 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-88  
                 Et 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 2-89  
                 Et 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 2-90  
                 Et 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 2-91  
                 Et 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 2-92  
                 Et 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 2-93  
                 Et 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-94  
                 Et 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-95  
                 Et 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-96  
                 Et 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 2-97  
                 Me 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 2-98 
                 Me 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 2-99 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 2-100 
                 Me 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 2-101  
                 Me 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-102  
                 Me 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-103 
                 Me 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-104 
                 Me 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-105 
                 Me 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 2-106 
                 Me 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 2-107 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 2-108 
                 Me 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 2-109 
                 Me 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-110 
                 Me 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-111 
                 Me 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-112 
                 Me 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-113 
                 Me 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 2-114 
                 Me 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 2-115 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 2-116 
                 Me 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 2-117 
                 Me 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-118 
                 Me 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-119 
                 Me 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-120 
                 Me 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-121 
                 Et 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 2-122 
                 Et 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 2-123 
                 Et 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 2-124 
                 Et 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 2-125 
                 Et 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-126 
                 Et 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-127 
                 Et 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-128 
                 Et 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 2-129 
                 Et 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 2-130 
                 Et 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 2-131 
                 Et 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 2-132 
                 Et 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 2-133 
                 Et 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-134 
                 Et 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-135 
                 Et 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-136 
                 Et 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 2-137 
                 Et 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 2-138 
                 Et 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 2-139 
                 Et 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 2-140 
                 Et 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 2-141 
                 Et 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-142 
                 Et 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-143 
                 Et 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-144 
                 Et 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 2-145 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                   
               
               
                 2-146 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 2-147 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 2-148 
                 Me 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 2-149 
                 Me 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-150 
                 Me 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-151 
                 Me 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-152 
                 Me 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-153 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                   
               
               
                 2-154 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 2-155 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 2-156 
                 Me 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 2-157 
                 Me 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-158 
                 Me 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-159 
                 Me 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-160 
                 Me 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-161 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                   
               
               
                 2-162 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 2-163 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 2-164 
                 Me 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 2-165 
                 Me 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-166 
                 Me 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-167 
                 Me 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-168 
                 Me 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-169 
                 Et 
                 Me 
                 0 
                 C 2 F 5   
                   
               
               
                 2-170 
                 Et 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 2-171 
                 Et 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 2-172 
                 Et 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 2-173 
                 Et 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-174 
                 Et 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-175 
                 Et 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-176 
                 Et 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 2-177 
                 Et 
                 Me 
                 1 
                 C 2 F 5   
                   
               
               
                 2-178 
                 Et 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 2-179 
                 Et 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 2-180 
                 Et 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 2-181 
                 Et 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-182 
                 Et 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-183 
                 Et 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-184  
                 Et 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 2-185 
                 Et 
                 Me 
                 2 
                 C 2 F 5   
                   
               
               
                 2-186  
                 Et 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 2-187 
                 Et 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 2-188  
                 Et 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 2-189 
                 Et 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-190 
                 Et 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-191 
                 Et 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-192 
                 Et 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 2-193 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-194 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-195 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-196 
                 Me 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-197 
                 Me 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-198 
                 Me 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-199 
                 Me 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-200 
                 Me 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-201 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-202 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-203 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-204 
                 Me 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-205 
                 Me 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-206 
                 Me 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-207 
                 Me 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-208 
                 Me 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-209 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-210 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-211 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-212 
                 Me 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-213 
                 Me 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-214 
                 Me 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-215 
                 Me 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-216 
                 Me 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-217 
                 Et 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-218 
                 Et 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-219 
                 Et 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-220 
                 Et 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-221 
                 Et 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-222 
                 Et 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-223 
                 Et 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-224 
                 Et 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 2-225 
                 Et 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-226 
                 Et 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-227 
                 Et 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-228 
                 Et 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-229 
                 Et 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-230 
                 Et 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-231 
                 Et 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-232 
                 Et 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 2-233 
                 Et 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-234 
                 Et 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-235 
                 Et 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-236 
                 Et 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-237 
                 Et 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-238 
                 Et 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-239 
                 Et 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-240 
                 Et 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 2-241 
                 Me 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 2-242 
                 Me 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 2-243 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 2-244 
                 Me 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 2-245 
                 Me 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-246 
                 Me 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-247 
                 Me 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-248 
                 Me 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-249 
                 Me 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 2-250 
                 Me 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 2-251 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 2-252  
                 Me 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 2-253  
                 Me 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-254  
                 Me 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-255  
                 Me 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-256  
                 Me 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-257  
                 Me 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 2-258  
                 Me 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 2-259  
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 2-260  
                 Me 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 2-261  
                 Me 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-262  
                 Me 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-263  
                 Me 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-264  
                 Me 
                 t-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-265  
                 Et 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 2-266  
                 Et 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 2-267  
                 Et 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 2-268  
                 Et 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 2-269  
                 Et 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-270  
                 Et 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-271  
                 Et 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-272  
                 Et 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 2-273  
                 Et 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 2-274  
                 Et 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 2-275  
                 Et 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 2-276  
                 Et 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 2-277  
                 Et 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-278  
                 Et 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-279  
                 Et 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-280  
                 Et 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 2-281  
                 Et 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 2-282  
                 Et 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 2-283  
                 Et 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 2-284  
                 Et 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 2-285  
                 Et 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-286  
                 Et 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-287  
                 Et 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 2-288 
                 Et 
                 t-Bu 
                 2 
                 CHF 2   
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 3 
               
             
            
               
                   
               
               
                 Inventive compounds of the formula (I) in which R 2  and R 3    
               
               
                 are methyl, and R 4  is hydrogen 
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
            
           
           
               
               
               
               
               
               
            
               
                   
                   
                   
                   
                   
                 Physical data: 
               
               
                 No. 
                 X 
                 R 1   
                 n 
                 Y 
                   1 H-NMR: δ [CDCl 3 ] 
               
               
                   
               
               
                 3-1 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-2 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-3 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-4 
                 Me 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-5 
                 Me 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-6 
                 Me 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-7 
                 Me 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-8 
                 Me 
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-9 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-10 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-11 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-12 
                 Me 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-13 
                 Me 
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-14 
                 Me 
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-15 
                 Me 
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-16 
                 Me 
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-17 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-18 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-19 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-20 
                 Me 
                 i-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-21 
                 Me 
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-22 
                 Me 
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-23 
                 Me 
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-24 
                 Me 
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-25 
                 Et 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-26 
                 Et 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-27 
                 Et 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-28 
                 Et 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-29 
                 Et 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-30 
                 Et 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-31 
                 Et 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-32 
                 Et  
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 3-33 
                 Et 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-34 
                 Et 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-35 
                 Et  
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-36 
                 Et 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-37 
                 Et  
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-38 
                 Et  
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-39 
                 Et  
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-40 
                 Et  
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 3-41 
                 Et 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-42 
                 Et 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-43 
                 Et  
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-44 
                 Et 
                 i-Pr  
                 2 
                 CF 2 Cl 
                   
               
               
                 3-45 
                 Et  
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-46 
                 Et  
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-47 
                 Et  
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-48 
                 Et  
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 3-49 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 3-50 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 3-51 
                 Me  
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 3-52 
                 Me 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 3-53 
                 Me  
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-54 
                 Me  
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-55 
                 Me  
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-56 
                 Me  
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-57 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 3-58 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 3-59 
                 Me  
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 3-60  
                 Me 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 3-61 
                 Me  
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-62 
                 Me 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-63 
                 Me 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-64 
                 Me 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-65 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 3-66  
                 Me 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 3-67 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 3-68 
                 Me 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 3-69 
                 Me 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-70 
                 Me 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-71 
                 Me 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-72 
                 Me 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-73 
                 Et 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 3-74 
                 Et 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 3-75 
                 Et 
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 3-76 
                 Et 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 3-77 
                 Et 
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-78 
                 Et 
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-79 
                 Et 
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-80 
                 Et 
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 3-81 
                 Et 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 3-82 
                 Et 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 3-83 
                 Et 
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 3-84 
                 Et 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 3-85 
                 Et 
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-86 
                 Et 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-87 
                 Et 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-88 
                 Et 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 3-89 
                 Et 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 3-90 
                 Et 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 3-91 
                 Et 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 3-92 
                 Et 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 3-93 
                 Et 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-94 
                 Et 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-95 
                 Et 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-96 
                 Et 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 3-97 
                 Me 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 3-98 
                 Me 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 3-99 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 3-100 
                 Me 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 3-101 
                 Me 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-102 
                 Me 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-103 
                 Me 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-104 
                 Me 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-105 
                 Me 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 3-106 
                 Me 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 3-107 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 3-108 
                 Me 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 3-109 
                 Me 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-110 
                 Me 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-111 
                 Me 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-112 
                 Me 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-113 
                 Me 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 3-114 
                 Me 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 3-115 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 3-116 
                 Me 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 3-117 
                 Me 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-118 
                 Me 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-119 
                 Me 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-120 
                 Me 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-121 
                 Et 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 3-122 
                 Et 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 3-123 
                 Et 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 3-124 
                 Et 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 3-125 
                 Et 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-126 
                 Et 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-127 
                 Et 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-128 
                 Et 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 3-129 
                 Et 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 3-130 
                 Et 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 3-131 
                 Et 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 3-132 
                 Et 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 3-133 
                 Et 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-134 
                 Et 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-135 
                 Et 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-136 
                 Et 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 3-137 
                 Et 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 3-138 
                 Et 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 3-139 
                 Et 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 3-140 
                 Et 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 3-141 
                 Et 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-142 
                 Et 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-143 
                 Et 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-144 
                 Et 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 3-145 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 7.62 (d, 1H), 7.31 (d, 1H), 3.64 (s, 3H),  
               
               
                   
                   
                   
                   
                   
                 2.61 (s, 3H), 2.28 (s, 3H), 1.63 (s, 3H) 
               
               
                 3-146 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 3-147 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 3-148 
                 Me 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 3-149 
                 Me 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-150 
                 Me 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-151 
                 Me 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-151 
                 Me 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-153 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 7.63 (d, 1H), 7.43 (d, 1H), 3.66 (s, 3H),  
               
               
                   
                   
                   
                   
                   
                 3.03 (s, 3H), 2.86 (s, 3H), 1.67 (s, 3H) 
               
               
                 3-154 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 3-155 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 3-156 
                 Me 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 3-157 
                 Me 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-158 
                 Me 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-159 
                 Me 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-160 
                 Me 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-161 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 7.77 (d, 1H), 7.53 (d, 1H), 3.66 (s, 3H),  
               
               
                   
                   
                   
                   
                   
                 3.28 (s, 3H), 2.72 (s, 3H), 1.68 (s, 3H) 
               
               
                 3-162 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 3-163 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 3-164 
                 Me 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 3-165 
                 Me 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-166 
                 Me 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-167 
                 Me 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-168 
                 Me 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-169 
                 Et 
                 Me 
                 0 
                 C 2 F 5   
                   
               
               
                 3-170 
                 Et 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 3-171 
                 Et 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 3-172 
                 Et 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 3-173 
                 Et 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-174 
                 Et 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-175 
                 Et 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-176 
                 Et 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 3-177 
                 Et 
                 Me 
                 1 
                 C 2 F 5   
                   
               
               
                 3-178 
                 Et 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 3-179 
                 Et 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 3-180 
                 Et 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 3-181 
                 Et 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-182 
                 Et 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-183 
                 Et 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-184 
                 Et 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 3-185 
                 Et 
                 Me 
                 2 
                 C 2 F 5   
                   
               
               
                 3-186 
                 Et 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 3-187 
                 Et 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 3-188 
                 Et 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 3-189 
                 Et 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-190 
                 Et 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-191 
                 Et 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-192 
                 Et 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 3-193 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-194 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-195 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-196 
                 Me 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-197 
                 Me 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-198 
                 Me 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-199 
                 Me 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-200 
                 Me 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-201 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-202 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-203 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-204 
                 Me 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-205 
                 Me 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-206 
                 Me 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-207 
                 Me 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-208 
                 Me 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-209 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-210 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-211 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-212 
                 Me 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-213 
                 Me 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-214 
                 Me 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-215 
                 Me 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-216 
                 Me 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-217 
                 Et 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-218 
                 Et 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-219 
                 Et 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-220 
                 Et 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-221 
                 Et 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-222 
                 Et 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-223 
                 Et 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-224 
                 Et 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 3-225 
                 Et 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-226 
                 Et 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-227 
                 Et 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-228 
                 Et 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-229 
                 Et 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-230 
                 Et 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-231 
                 Et 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-232 
                 Et 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 3-233 
                 Et 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-234 
                 Et 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-235 
                 Et 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-236 
                 Et 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-237 
                 Et 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-238 
                 Et 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-239 
                 Et 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-240 
                 Et 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 3-241 
                 Me 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 3-242 
                 Me 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 3-243 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 3-244 
                 Me 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 3-245 
                 Me 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-246 
                 Me 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-247 
                 Me 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-248 
                 Me 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-249 
                 Me 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 3-250 
                 Me 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 3-251 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 3-252 
                 Me 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 3-253 
                 Me 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-254 
                 Me 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-255 
                 Me 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-256 
                 Me 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-257 
                 Me 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 3-258 
                 Me 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 3-259 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 3-260 
                 Me 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 3-261 
                 Me 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-262 
                 Me 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-263 
                 Me 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-264 
                 Me 
                 t-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-265 
                 Et 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 3-266 
                 Et 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 3-267 
                 Et 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 3-268 
                 Et 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 3-269 
                 Et 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-270  
                 Et 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-271 
                 Et 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-272 
                 Et 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 3-273 
                 Et 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 3-274 
                 Et 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 3-275 
                 Et 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 3-276 
                 Et 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 3-277 
                 Et 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-278 
                 Et 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-279 
                 Et 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-280 
                 Et 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 3-281 
                 Et 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 3-282 
                 Et 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 3-283 
                 Et 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 3-284 
                 Et 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 3-285 
                 Et 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-286 
                 Et 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-287 
                 Et 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 3-288 
                 Et 
                 t-Bu 
                 2 
                 CHF 2   
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 4 
               
             
            
               
                   
               
               
                 Inventive compounds of the formula (I) 
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
            
           
           
               
               
               
               
               
               
               
               
               
            
               
                   
                   
                   
                   
                   
                   
                   
                   
                 Physical data:  
               
               
                 No. 
                 R 2   
                 R 3   
                 X 
                 R 1   
                 n 
                 Y 
                 R 4   
                   1 H-NMR: δ [CDCl 3 ] 
               
               
                   
               
               
                 4-1 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-2 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-3 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-4 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-5 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-6 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-7 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-8 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-9 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 -n-Pr 
                   
               
               
                 4-10 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-11 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-12 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-13 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-14 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-15 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-16 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-17 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-18 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-19 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-20 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-21 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-22 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-23 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-24 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-25 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-26 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-27 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-28 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 -(4-Me—Ph) 
                   
               
               
                 4-29 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 -(4-Me—Ph) 
                   
               
               
                 4-30 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 -(4-Me—Ph) 
                   
               
               
                 4-31 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 -(4-Me—Ph) 
                   
               
               
                 4-32 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 -—(4-Me—Ph) 
                   
               
               
                 4-33 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 -(4-Me—Ph) 
                   
               
               
                 4-34 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 -(4-Me—Ph) 
                   
               
               
                 4-35 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 -—(4-Me—Ph) 
                   
               
               
                 4-36 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 -—(4-Me—Ph) 
                   
               
               
                 4-37 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-38 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-39 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-40 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-41 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-42 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-43 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-44 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-45 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-46 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-47 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-48 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-49 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-50 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-51 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-52 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-53 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-54 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-55 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-56 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-57 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-58 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-59 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-60 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-61 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-62 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-63 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-64 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-65 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-66 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-67 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-68 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-69 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-70 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-71 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-72 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-73 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-74 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-75 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-76 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-77 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-78 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-79 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-80 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-81 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-82 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-83 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-84 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-85 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-86 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-87 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-88 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-89 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-90 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-91 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-92 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-93 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-94 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-95 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-96 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-97 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-98 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-99 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-100 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-101 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-102 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-103 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-104 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-105 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-106 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-107 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-108 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-109 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-110 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-111 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-112 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-113 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-114 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-115 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-116 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-117 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-118 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-119 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-120 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-121 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-122 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-123 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-124 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-125 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-126 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-127 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-128 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-129 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-130 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-131 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-132 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-133 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-134 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-135 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —n-Pr 
                   
               
               
                 4-136 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-137 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-138 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-139 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-140 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-141 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-142 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-143 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-144 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-145 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-146 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-147 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-148 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-149 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-150 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-151 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-152 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-153 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —Ph 
                   
               
               
                 4-154 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-155 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-156 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-157 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-158 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-159 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-160 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-161 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-162 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-163 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-164 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-165 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-166 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-167 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-168 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-169 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-170 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-171 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-172 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-173 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-174 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-175 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-176 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-177 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-178 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-179 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-180 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —CO—Ph 
                   
               
               
                 4-181 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-182 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-183 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-184 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-185 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-186 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-187 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-188 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-189 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                 —CH 2 —CO—Ph 
                   
               
               
                 4-190 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-191 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-192 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-193 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-194 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-195 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-196 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-197 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-198 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-199 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-200 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-201 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-202 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-203 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-204 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-205 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-206 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-207 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-208 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-209 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-210 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-211 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-212 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-213 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-214 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-215 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-216 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-217 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-218 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-219 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-220 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-221 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-222 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-223 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-224 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-225 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-226 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-227 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-228 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-229 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-230 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-231 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-232 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-233 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-234 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-235 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-236 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-237 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-238 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-239 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-240 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-241 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-242 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-243 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-244 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-245 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-246 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-247 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-248 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-249 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-250 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-251 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-252 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-253 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-254 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-255 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-256 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-257 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-258 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-259 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-260 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-261 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-262 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-263 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-264 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-265 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-266 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-267 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-268 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-269 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-270 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-271 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-272 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-273 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-274 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-275 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-276 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-277 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-278 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-279 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-280 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-281 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-282 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-283 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-284 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-285 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-286 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-287 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-288 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-289 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-290 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-291 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-292 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-293 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-294 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-295 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-296 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-297 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-298 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-299 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-300 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-301 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-302 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-303 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-304 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-305 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-306 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-307 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-308 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-309 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-310 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-311 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-312 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-313 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-314 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-315 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-316 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-317 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-318 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-319 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-320 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-321 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-322 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-323 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-324 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-325 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-326 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-327 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-328 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-329 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-330 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-331 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-332 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-333 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-334 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-335 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-336 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-337 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-338 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-339 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-340 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-341 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-342 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —Ph 
                   
               
               
                 4-343 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-344 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-345 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-346 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-347 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-348 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-349 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-350 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-351 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-352 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-353 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-354 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-355 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-356 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-357 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-358 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-359 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-360 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-361 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-362 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-363 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-364 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-365 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-366 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-367 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-368 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-369 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —CO—Ph 
                   
               
               
                 4-370 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-371 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-372 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-373 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-374 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-375 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-376 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-377 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-378 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-379 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-380 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-381 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-382 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-383 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-384 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-385 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-386 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-387 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-388 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-389 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-390 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-391 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-392 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-393 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-394 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-395 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-396 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-397 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-398 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-399 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-400 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-401 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-402 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-403 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-404 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-405 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-406 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-407 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-408 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-409 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-410 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-411 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-412 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-413 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-414 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-415 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-416 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-417 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-418 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-419 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-420 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-421 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-422 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-423 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-424 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-425 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-426 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-427 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-428 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-429 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-430 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-431 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-432 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-433 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-434 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-435 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-436 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-437 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-438 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-439 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-440 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-441 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-442 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-443 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-444 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-445 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-446 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-447 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-448 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-449 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-450 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-451 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-452 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-453 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-454 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-455 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-456 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-457 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-458 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-459 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-460 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-461 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-462 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-463 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-464 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-465 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-466 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-467 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-468 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-469 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-470 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-471 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-472 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-473 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-474 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-475 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-476 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-477 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-478 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-479 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-480 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-481 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-482 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-483 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-484 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-485 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-486 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-487 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-488 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-489 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-490 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-491 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-492 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-493 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-494 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-495 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-496 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-497 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-498 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-499 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-500 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-501 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-502 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-503 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-504 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-505 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-506 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-507 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-508 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-509 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-510 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-511 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-512 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-513 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —n-Pr 
                   
               
               
                 4-514 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-515 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-516 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-517 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-518 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-519 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-520 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-521 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-522 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-523 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-524 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-525 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-526 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-527 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-528 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-529 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-530 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-531 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —Ph 
                   
               
               
                 4-532 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-533 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-534 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-535 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-536 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-537 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-538 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-539 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-540 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-541 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-542 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-543 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-544 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-545 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-546 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-547 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-548 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-549 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-550 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-551 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-552 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-553 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-554 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-555 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-556 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-557 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-558 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —CO—Ph 
                   
               
               
                 4-559 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-560 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-561 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-562 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-563 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-564 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-565 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-566 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-567 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-568 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-569 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-570 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-571 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-572 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-573 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-574 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-575 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-576 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-577 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-578 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-579 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-580 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-581 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-582 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-583 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-584 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-585 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-586 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-587 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-588 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-589 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-590 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-591 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-592 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-593 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-594 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-595 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-596 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-597 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-598 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-599 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-600 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-601 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-602 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-603 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-604 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-605 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-606 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-607 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-608 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-609 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-610 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-611 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-612 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-613 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-614 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-615 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-616 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-617 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-618 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-619 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-620 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-621 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-622 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-623 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-624 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-625 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-626 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-627 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-628 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-629 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-630 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-631 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-632 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-633 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-634 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-635 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-636 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-637 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-638 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-639 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-640 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-641 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-642 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-643 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-644 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-645 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-646 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-647 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-648 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-649 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-650 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-651 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-652 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-653 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-654 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-655 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-656 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-657 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-658 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-659 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-660 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-661 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-662 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-663 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-664 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-665 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-666 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-667 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-668 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-669 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-670 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-671 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-672 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-673 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-674 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-675 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-676 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-677 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-678 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-679 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-680 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-681 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-682 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-683 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-684 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-685 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-686 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-687 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-688 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-689 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-690 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-691 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-692 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-693 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-694 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-695 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-696 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-697 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-698 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-699 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-700 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-701 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-702 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —n-Pr 
                   
               
               
                 4-703 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-704 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-705 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-706 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-707 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-708 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-709 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-710 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-711 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-712 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-713 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-714 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-715 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-716 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-717 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-718 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-719 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-720 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —Ph 
                   
               
               
                 4-721 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-722 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-723 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-724 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-725 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-726 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-727 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-728 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-729 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-730 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-731 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-732 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-733 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-734 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-735 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-736 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-737 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-738 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-739 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-740 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-741 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-742 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-743 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-744 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-745 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-746 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-747 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —CO—Ph 
                   
               
               
                 4-748 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-749 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-750 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-751 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-752 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-753 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-754 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-755 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-756 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-757 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-758 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-759 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-760 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-761 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-762 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-763 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-764 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-765 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-766 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-767 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-768 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-769 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-770 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-771 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-772 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-773 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-774 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-775 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-776 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-777 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-778 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-779 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-780 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-781 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-782 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-783 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-784 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-785 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-786 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-787 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-788 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-789 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-790 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-791 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-792 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-793 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-794 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-795 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-796 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-797 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-798 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-799 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-800 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-801 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-802 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-803 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-804 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-805 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-806 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-807 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-808 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-809 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-810 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-811 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-812 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-813 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-814 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-815 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-816 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-817 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-818 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-819 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-820 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-821 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-822 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-823 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-824 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-825 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-826 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-827 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-828 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-829 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-830 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-831 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-832 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-833 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-834 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-835 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-836 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-837 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-838 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-839 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-840 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-841 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-842 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-843 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-844 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-845 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-846 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-847 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-848 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-849 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-850 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-851 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-852 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-853 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-854 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-855 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-856 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-857 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-858 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-859 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-860 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-861 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-862 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-863 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-864 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-865 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-866 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-867 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-868 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-869 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-870 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-871 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-872 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-873 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-874 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-875 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-876 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-877 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-878 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-879 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-880 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-881 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-882 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-883 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-884 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-885 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-886 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-887 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-888 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-889 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-890 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-891 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-892 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-893 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-894 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-895 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-896 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-897 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-898 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-899 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-900 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-901 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-902 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-903 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-904 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-905 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-906 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-907 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-908 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-909 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —Ph 
                   
               
               
                 4-910 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-911 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-912 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-913 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-914 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-915 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-916 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-917 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-918 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-919 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-920 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-921 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-922 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-923 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-924 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-925 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-926 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-927 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-928 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-929 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-930 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-931 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-932 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-933 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-934 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-935 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-936 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —CO—Ph 
                   
               
               
                 4-937 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-938 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-939 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-940 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-941 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-942 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-943 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-944 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-945 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-946 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-947 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-948 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-949 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-950 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-951 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-952 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-953 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-954 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-955 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-956 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-957 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-958 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-959 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-960 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-961 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-962 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-963 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-964 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-965 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-966 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-967 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-968 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-969 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-970 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-971 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-972 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-973 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-974 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-975 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-976 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-977 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-978 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-979 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-980 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-981 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-982 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-983 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-984 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-985 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-986 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-987 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-988 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-989 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-990 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-991 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-992 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-993 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-994 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-995 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-996 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-997 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-998 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-999 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1000 
                 Me 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1001 
                 Me 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1002 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1003 
                 Me 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1004 
                 Me 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1005 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1006 
                 Me 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1007 
                 Me 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1008 
                 Me 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1009 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1010 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1011 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1012 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1013 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1014 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1015 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1016 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1017 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1018 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1019 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1020 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1021 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1022 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1023 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1024 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1025 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1026 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1027 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1028 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1029 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1030 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1031 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1032 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1033 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1034 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1035 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1036 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1037 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1038 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1039 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1040 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1041 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1042 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1043 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1044 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1045 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1046 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1047 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1048 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1049 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1050 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1051 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1052 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1053 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1054 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1055 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1056 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1057 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1058 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1059 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1060 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1061 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1062 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1063 
                 Et 
                 H 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1064 
                 Et 
                 H 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1065 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1066 
                 Et 
                 H 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1067 
                 Et 
                 H 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1068 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1069 
                 Et 
                 H 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1070 
                 Et 
                 H 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1071 
                 Et 
                 H 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1072 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1073 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1074 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1075 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1076 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1077 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1078 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1079 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1080 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —n-Pr 
                   
               
               
                 4-1081 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1082 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1083 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1084 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1085 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1086 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1087 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1088 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1089 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —(CH 2 ) 2 OMe 
                   
               
               
                 4-1090 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1091 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1092 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1093 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1094 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1095 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1096 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1097 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1098 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —Ph 
                   
               
               
                 4-1099 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1100 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1101 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1102 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1103 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1104 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1105 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1106 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1107 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 —(4-Me—Ph) 
                   
               
               
                 4-1108 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1109 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1110 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1111 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1112 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1113 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1114 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1115 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1116 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —SO 2 -(Thien-2-yl) 
                   
               
               
                 4-1117 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1118 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1119 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1120 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1121 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1122 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1123 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1124 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1125 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —CO—Ph 
                   
               
               
                 4-1126 
                 Me 
                 Me 
                 Me 
                 Me 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1127 
                 Me 
                 Me 
                 Me 
                 Et 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1128 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1129 
                 Me 
                 Me 
                 Me 
                 Me 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1130 
                 Me 
                 Me 
                 Me 
                 Et 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1131 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1132 
                 Me 
                 Me 
                 Me 
                 Me 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1133 
                 Me 
                 Me 
                 Me 
                 Et 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
                   
               
               
                 4-1134 
                 Me 
                 Me 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                 —CH 2 —CO—Ph 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
             
               
                 TABLE 5 
               
               
                   
               
             
            
               
                 Inventive compounds of the formula (IIIa), 
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
            
           
           
               
               
               
               
               
               
            
               
                 No. 
                 X 
                 R 1   
                 n 
                 Y 
                 Physical data:  1 H-NMR: δ [DMSO-d 6 ] 
               
               
                   
               
               
                 5-1 
                 Me 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-2 
                 Me 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-3 
                 Me 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-4 
                 Me 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-5 
                 Me 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-6 
                 Me 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-7 
                 Me 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-8 
                 Me 
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-9 
                 Me 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-10 
                 Me 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-11 
                 Me 
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-12 
                 Me 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-13 
                 Me 
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-14 
                 Me 
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-15 
                 Me 
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-16 
                 Me 
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-17 
                 Me 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-18 
                 Me 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-19 
                 Me 
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-20 
                 Me 
                 i-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-21 
                 Me 
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-22 
                 Me 
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-23 
                 Me 
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-24 
                 Me 
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-25 
                 Et 
                 Me 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-26 
                 Et 
                 Et 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-27 
                 Et 
                 n-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-28 
                 Et 
                 i-Pr 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-29 
                 Et 
                 n-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-30 
                 Et 
                 i-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-31 
                 Et 
                 s-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-32 
                 Et 
                 t-Bu 
                 0 
                 CF 2 Cl 
                   
               
               
                 5-33 
                 Et 
                 Me 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-34 
                 Et 
                 Et 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-35 
                 Et 
                 n-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-36 
                 Et 
                 i-Pr 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-37 
                 Et 
                 n-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-38 
                 Et 
                 i-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-39 
                 Et 
                 s-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-40 
                 Et 
                 t-Bu 
                 1 
                 CF 2 Cl 
                   
               
               
                 5-41 
                 Et 
                 Me 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-42 
                 Et 
                 Et 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-43 
                 Et 
                 n-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-44 
                 Et 
                 i-Pr 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-45 
                 Et 
                 n-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-46 
                 Et 
                 i-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-47 
                 Et 
                 s-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-48 
                 Et 
                 t-Bu 
                 2 
                 CF 2 Cl 
                   
               
               
                 5-49 
                 Me 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 5-50 
                 Me 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 5-51 
                 Me 
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 5-52 
                 Me 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 5-53 
                 Me 
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-54 
                 Me 
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-55 
                 Me 
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-56 
                 Me 
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-57 
                 Me 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 5-58 
                 Me 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 5-59 
                 Me 
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 5-60 
                 Me 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 5-61 
                 Me 
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-62 
                 Me 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-63 
                 Me 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-64 
                 Me 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-65 
                 Me 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 5-66 
                 Me 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 5-67 
                 Me 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 5-68 
                 Me 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 5-69 
                 Me 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-70 
                 Me 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-71 
                 Me 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-72 
                 Me 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-73 
                 Et 
                 Me 
                 0 
                 CFCl 2   
                   
               
               
                 5-74 
                 Et 
                 Et 
                 0 
                 CFCl 2   
                   
               
               
                 5-75 
                 Et 
                 n-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 5-76 
                 Et 
                 i-Pr 
                 0 
                 CFCl 2   
                   
               
               
                 5-77 
                 Et 
                 n-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-78 
                 Et 
                 i-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-79 
                 Et 
                 s-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-80 
                 Et 
                 t-Bu 
                 0 
                 CFCl 2   
                   
               
               
                 5-81 
                 Et 
                 Me 
                 1 
                 CFCl 2   
                   
               
               
                 5-82 
                 Et 
                 Et 
                 1 
                 CFCl 2   
                   
               
               
                 5-83 
                 Et 
                 n-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 5-84 
                 Et 
                 i-Pr 
                 1 
                 CFCl 2   
                   
               
               
                 5-85 
                 Et 
                 n-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-86 
                 Et 
                 i-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-87 
                 Et 
                 s-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-88 
                 Et 
                 t-Bu 
                 1 
                 CFCl 2   
                   
               
               
                 5-89 
                 Et 
                 Me 
                 2 
                 CFCl 2   
                   
               
               
                 5-90 
                 Et 
                 Et 
                 2 
                 CFCl 2   
                   
               
               
                 5-91 
                 Et 
                 n-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 5-92 
                 Et 
                 i-Pr 
                 2 
                 CFCl 2   
                   
               
               
                 5-93 
                 Et 
                 n-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-94 
                 Et 
                 i-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-95 
                 Et 
                 s-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-96 
                 Et 
                 t-Bu 
                 2 
                 CFCl 2   
                   
               
               
                 5-97 
                 Me 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 5-98 
                 Me 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 5-99 
                 Me 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 5-100 
                 Me 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 5-101 
                 Me 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-102 
                 Me 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-103 
                 Me 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-104 
                 Me 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-105 
                 Me 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 5-106 
                 Me 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 5-107 
                 Me 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 5-108 
                 Me 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 5-109 
                 Me 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-110 
                 Me 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-111 
                 Me 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-112 
                 Me 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-113 
                 Me 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 5-114 
                 Me 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 5-115 
                 Me 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 5-116 
                 Me 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 5-117 
                 Me 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-118 
                 Me 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-119 
                 Me 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-120 
                 Me 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-121 
                 Et 
                 Me 
                 0 
                 CCl 3   
                   
               
               
                 5-122 
                 Et 
                 Et 
                 0 
                 CCl 3   
                   
               
               
                 5-123 
                 Et 
                 n-Pr 
                 0 
                 CCl 3   
                   
               
               
                 5-124 
                 Et 
                 i-Pr 
                 0 
                 CCl 3   
                   
               
               
                 5-125 
                 Et 
                 n-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-126 
                 Et 
                 i-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-127 
                 Et 
                 s-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-128 
                 Et 
                 t-Bu 
                 0 
                 CCl 3   
                   
               
               
                 5-129 
                 Et 
                 Me 
                 1 
                 CCl 3   
                   
               
               
                 5-130 
                 Et 
                 Et 
                 1 
                 CCl 3   
                   
               
               
                 5-131 
                 Et 
                 n-Pr 
                 1 
                 CCl 3   
                   
               
               
                 5-132 
                 Et 
                 i-Pr 
                 1 
                 CCl 3   
                   
               
               
                 5-133 
                 Et 
                 n-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-134 
                 Et 
                 i-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-135 
                 Et 
                 s-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-136 
                 Et 
                 t-Bu 
                 1 
                 CCl 3   
                   
               
               
                 5-137 
                 Et 
                 Me 
                 2 
                 CCl 3   
                   
               
               
                 5-138 
                 Et 
                 Et 
                 2 
                 CCl 3   
                   
               
               
                 5-139 
                 Et 
                 n-Pr 
                 2 
                 CCl 3   
                   
               
               
                 5-140 
                 Et 
                 i-Pr 
                 2 
                 CCl 3   
                   
               
               
                 5-141 
                 Et 
                 n-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-142 
                 Et 
                 i-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-143 
                 Et 
                 s-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-144 
                 Et 
                 t-Bu 
                 2 
                 CCl 3   
                   
               
               
                 5-145 
                 Me 
                 Me 
                 0 
                 C 2 F 5   
                 7.84 (d, 1H), 7.65 (d, 1H), 
               
               
                   
                   
                   
                   
                   
                 2.76 (s, 3H), 2.27 (s, 3H) 
               
               
                 5-146 
                 Me 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 5-147 
                 Me 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 5-148 
                 Me 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 5-149 
                 Me 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-150 
                 Me 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-151 
                 Me 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-152 
                 Me 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-153 
                 Me 
                 Me 
                 1 
                 C 2 F 5   
                   
               
               
                 5-154 
                 Me 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 5-155 
                 Me 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 5-156 
                 Me 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 5-157 
                 Me 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-158 
                 Me 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-159 
                 Me 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-160 
                 Me 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-161 
                 Me 
                 Me 
                 2 
                 C 2 F 5   
                 8.03 (d, 1H), 7.82 (d, 1H), 
               
               
                   
                   
                   
                   
                   
                 3.44 (s, 3H), 2.74 (s, 3H) 
               
               
                 5-162 
                 Me 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 5-163 
                 Me 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 5-164 
                 Me 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 5-165 
                 Me 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-166 
                 Me 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-167 
                 Me 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-168 
                 Me 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-169 
                 Et 
                 Me 
                 0 
                 C 2 F 5   
                   
               
               
                 5-170 
                 Et 
                 Et 
                 0 
                 C 2 F 5   
                   
               
               
                 5-171 
                 Et 
                 n-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 5-172 
                 Et 
                 i-Pr 
                 0 
                 C 2 F 5   
                   
               
               
                 5-173 
                 Et 
                 n-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-174 
                 Et 
                 i-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-175 
                 Et 
                 s-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-176 
                 Et 
                 t-Bu 
                 0 
                 C 2 F 5   
                   
               
               
                 5-177 
                 Et 
                 Me 
                 1 
                 C 2 F 5   
                   
               
               
                 5-178 
                 Et 
                 Et 
                 1 
                 C 2 F 5   
                   
               
               
                 5-179 
                 Et 
                 n-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 5-180 
                 Et 
                 i-Pr 
                 1 
                 C 2 F 5   
                   
               
               
                 5-181 
                 Et 
                 n-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-182 
                 Et 
                 i-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-183 
                 Et 
                 s-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-184 
                 Et 
                 t-Bu 
                 1 
                 C 2 F 5   
                   
               
               
                 5-185 
                 Et 
                 Me 
                 2 
                 C 2 F 5   
                   
               
               
                 5-186 
                 Et 
                 Et 
                 2 
                 C 2 F 5   
                   
               
               
                 5-187 
                 Et 
                 n-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 5-188 
                 Et 
                 i-Pr 
                 2 
                 C 2 F 5   
                   
               
               
                 5-189 
                 Et 
                 n-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-190 
                 Et 
                 i-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-191 
                 Et 
                 s-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-192 
                 Et 
                 t-Bu 
                 2 
                 C 2 F 5   
                   
               
               
                 5-193 
                 Me 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-194 
                 Me 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-195 
                 Me 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-196 
                 Me 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-197 
                 Me 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-198 
                 Me 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-199 
                 Me 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-200 
                 Me 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-201 
                 Me 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-202 
                 Me 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-203 
                 Me 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-204 
                 Me 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-205 
                 Me 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-206 
                 Me 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-207 
                 Me 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-208 
                 Me 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-209 
                 Me 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-210 
                 Me 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-211 
                 Me 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-212 
                 Me 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-213 
                 Me 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-214 
                 Me 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-215 
                 Me 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-216 
                 Me 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-217 
                 Et 
                 Me 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-218 
                 Et 
                 Et 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-219 
                 Et 
                 n-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-220 
                 Et 
                 i-Pr 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-221 
                 Et 
                 n-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-222 
                 Et 
                 i-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-223 
                 Et 
                 s-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-224 
                 Et 
                 t-Bu 
                 0 
                 CF(CF 3 ) 2   
                   
               
               
                 5-225 
                 Et 
                 Me 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-226 
                 Et 
                 Et 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-227 
                 Et 
                 n-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-228 
                 Et 
                 i-Pr 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-229 
                 Et 
                 n-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-230 
                 Et 
                 i-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-231 
                 Et 
                 s-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-232 
                 Et 
                 t-Bu 
                 1 
                 CF(CF 3 ) 2   
                   
               
               
                 5-233 
                 Et 
                 Me 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-234 
                 Et 
                 Et 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-235 
                 Et 
                 n-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-236 
                 Et 
                 i-Pr 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-237 
                 Et 
                 n-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-238 
                 Et 
                 i-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-239 
                 Et 
                 s-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-240 
                 Et 
                 t-Bu 
                 2 
                 CF(CF 3 ) 2   
                   
               
               
                 5-241 
                 Me 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 5-242 
                 Me 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 5-243 
                 Me 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 5-244 
                 Me 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 5-245 
                 Me 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-246 
                 Me 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-247 
                 Me 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-248 
                 Me 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-249 
                 Me 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 5-250 
                 Me 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 5-251 
                 Me 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 5-252 
                 Me 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 5-253 
                 Me 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-254 
                 Me 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-255 
                 Me 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-256 
                 Me 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-257 
                 Me 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 5-258 
                 Me 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 5-259 
                 Me 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 5-260 
                 Me 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 5-261 
                 Me 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-262 
                 Me 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-263 
                 Me 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-264 
                 Me 
                 t-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-265 
                 Et 
                 Me 
                 0 
                 CHF 2   
                   
               
               
                 5-266 
                 Et 
                 Et 
                 0 
                 CHF 2   
                   
               
               
                 5-267 
                 Et 
                 n-Pr 
                 0 
                 CHF 2   
                   
               
               
                 5-268 
                 Et 
                 i-Pr 
                 0 
                 CHF 2   
                   
               
               
                 5-269 
                 Et 
                 n-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-270 
                 Et 
                 i-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-271 
                 Et 
                 s-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-272 
                 Et 
                 t-Bu 
                 0 
                 CHF 2   
                   
               
               
                 5-273 
                 Et 
                 Me 
                 1 
                 CHF 2   
                   
               
               
                 5-274 
                 Et 
                 Et 
                 1 
                 CHF 2   
                   
               
               
                 5-275 
                 Et 
                 n-Pr 
                 1 
                 CHF 2   
                   
               
               
                 5-276 
                 Et 
                 i-Pr 
                 1 
                 CHF 2   
                   
               
               
                 5-277 
                 Et 
                 n-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-278 
                 Et 
                 i-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-279 
                 Et 
                 s-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-280 
                 Et 
                 t-Bu 
                 1 
                 CHF 2   
                   
               
               
                 5-281 
                 Et 
                 Me 
                 2 
                 CHF 2   
                   
               
               
                 5-282 
                 Et 
                 Et 
                 2 
                 CHF 2   
                   
               
               
                 5-283 
                 Et 
                 n-Pr 
                 2 
                 CHF 2   
                   
               
               
                 5-284 
                 Et 
                 i-Pr 
                 2 
                 CHF 2   
                   
               
               
                 5-285 
                 Et 
                 n-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-286 
                 Et 
                 i-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-287 
                 Et 
                 s-Bu 
                 2 
                 CHF 2   
                   
               
               
                 5-288 
                 Et 
                 t-Bu 
                 2 
                 CHF 2   
               
               
                   
               
            
           
         
       
     
     B. Formulation Examples 
     1. Dust 
     A dust is obtained by mixing 10 parts by weight of a compound of the formula (I) and 90 parts by weight of talc as inert substance and comminuting the mixture in a hammer mill. 
     2. Dispersible Powder 
     A wettable powder which is readily dispersible in water is obtained by mixing 25 parts by weight of a compound of the formula (I), 64 parts by weight of kaolin-containing quartz as inert substance, 10 parts by weight of potassium lignosulfonate and 1 part by weight of sodium oleoylmethyltaurinate as wetting agent and dispersant, and grinding the mixture in a pinned-disk mill. 
     3. Dispersible Concentrate 
     A readily water-dispersible dispersion concentrate is obtained by mixing 20 parts by weight of a compound of the formula (I) with 6 parts by weight of alkylphenol polyglycol ether (®Triton X 207), 3 parts by weight of isotridecanol polyglycol ether (8 EO) and 71 parts by weight of paraffinic mineral oil (boiling range for example about 255 to above 277° C.) and grinding the mixture in a ball mill to a fineness of below 5 microns. 
     4. Emulsifiable Concentrate 
     An emulsifiable concentrate is obtained from 15 parts by weight of a compound of the formula (I), 75 parts by weight of cyclohexanone as solvent and 10 parts by weight of oxethylated nonylphenol as emulsifier. 
     5. Water-Dispersible Granules
     Water-dispersible granules are obtained by mixing   75 parts by weight of a compound of the formula (I),   10 parts by weight of calcium lignosulfonate,   5 parts by weight of sodium lauryl sulfate,   3 parts by weight of polyvinyl alcohol and   7 parts by weight of kaolin,   grinding the mixture in a pinned-disk mill, and granulating the powder in a fluidized bed by spraying on water as granulating liquid.   

     Water-dispersible granules are also obtained by homogenizing and precomminuting, in a colloid mill,
     25 parts by weight of a compound of the formula (I),   5 parts by weight of sodium 2,2′-dinaphthylmethane-6,6′-disulfonate,   2 parts by weight of sodium oleoylmethyltaurinate,   1 part by weight of polyvinyl alcohol,   17 parts by weight of calcium carbonate and   50 parts by weight of water,
 
subsequently grinding the mixture in a bead mill and atomizing and drying the resulting suspension in a spray tower by means of a single-fluid nozzle.
   

     C. Biological Examples 
     1. Pre-Emergence Herbicidal Action Against Weed Plants 
     Seeds or rhizome sections of mono- and dicotyledonous weed plants are set out in pots of 9 to 13 cm in diameter, in sandy loam soil, and are covered with soil. The herbicides, formulated as emulsifiable concentrates or dusts, are applied to the surface of the covering earth in the form of aqueous dispersions or suspensions or emulsions, at a water application rate of 300 to 800 I/ha (converted) in different doses. The pots are then maintained under glass under optimum conditions for the further cultivation of the plants. After 3 to 4 weeks under optimum growth conditions under glass, the trial plants are scored for the effect of the compounds according to the invention in comparison to compounds disclosed in the prior art. As the results in the comparison tables show, the selected compounds according to the invention exhibit a better herbicidal activity against a broad spectrum of economically important monocotyledonous and dicotyledonous weeds than the compounds disclosed in the prior art. 
     The meanings of the abbreviations used in the comparison tables below are as follows: 
     
       
         
           
               
               
               
               
             
               
                   
               
             
            
               
                 ALOMY 
                 
                   Alopecurus 
                 
                 AMARE 
                 
                   Amaranthus 
                 
               
               
                   
                 
                   myosuroides 
                 
                   
                 
                   retroflexus 
                 
               
               
                 AVEFA 
                 
                   Avena fatua 
                 
                 CYPES 
                 
                   Cyperus serotinus 
                 
               
               
                 MATIN 
                 
                   Matricaria inodora 
                 
                 SETVI 
                 
                   Setaria viridis 
                 
               
               
                 VIOTR 
                 
                   Viola tricolor 
                 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
            
               
                   
               
               
                 Comparison table 1: Pre-emergence 
               
            
           
           
               
               
               
            
               
                   
                   
                 Herbicidal action against 
               
            
           
           
               
               
               
               
               
            
               
                 Compound 
                 Dose [g a.c./ha] 
                 AVEFA 
                 CYPES 
                 VIOTR 
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80 
                 70% 
                 100% 
                 90% 
               
               
                   
               
               
                 inventive compound No. 1-153 
                   
                   
                   
                   
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80 
                 40% 
                  50% 
                 60% 
               
               
                   
               
               
                 compound No. 1-9, known from 
                   
                   
                   
                   
               
               
                 WO 2008/125214 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
            
               
                   
               
               
                 Comparison table 2: Pre-emergence 
               
            
           
           
               
               
               
            
               
                   
                 Dose 
                 Herbicidal 
               
               
                   
                 [g a.c./ 
                 action against 
               
            
           
           
               
               
               
               
            
               
                 Compound 
                 ha] 
                 ALOMY 
                 CYPES 
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 320 
                 90% 
                 80% 
               
               
                   
               
               
                 inventive compound No. 3-161 
                   
                   
                   
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 320 
                 50% 
                 50% 
               
               
                   
               
               
                 compound No. 3-17, known from 
                   
                   
                   
               
               
                 WO 2008/125214 
               
               
                   
               
            
           
         
       
     
                            Comparison table 3: Pre-emergence                                 Herbicidal           Dose   action against       Compound   [g a.c./ha]   VIOTR                                     320   90%               inventive compound No. 3-153                                             320   40%               compound No. 3-9, known from               WO 2008/125214                    
2. Post-Emergence Herbicidal Action Against Weed Plants
 
Seeds of monocotyledonous and dicotyledonous weed plants are set out in cardboard pots in sandy loam soil, covered with soil, and cultivated under glass under good growth conditions. Two to three weeks after sowing, the trial plants are treated at the three-leaf stage. The compounds according to the invention, formulated as wettable powders or as emulsifiable concentrates, are sprayed onto the surface of the green parts of the plants, at a water application rate of 600 to 800 I/ha (converted). After the trial plants have stood for 3 to 4 weeks under optimum growth conditions under glass, the action of the compounds according to the invention is scored in comparison to compounds disclosed in the prior art. As the results in the comparison tables show, the selected compounds according to the invention exhibit a better herbicidal activity against a broad spectrum of economically important monocotyledonous and dicotyledonous weeds than the compounds disclosed in the prior art.
 
     
       
         
           
               
            
               
                   
               
               
                 Comparison table 4: Post-emergence 
               
            
           
           
               
               
               
            
               
                   
                   
                 Herbicidal 
               
               
                   
                 Dose 
                 action against 
               
               
                 Compound 
                 [g a.c./ha] 
                 MATIN 
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80  
                 100% 
               
               
                   
               
               
                 inventive compound No. 1-161 
                   
                   
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80 
                  50% 
               
               
                   
               
               
                 compound No. 1-4, known from 
                   
                   
               
               
                 WO 2008/125214 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
            
               
                   
               
               
                 Comparison table 5: Post-emergence 
               
            
           
           
               
               
               
            
               
                   
                 Dose 
                 Herbicidal 
               
               
                   
                 [g a.c./ 
                 action against 
               
            
           
           
               
               
               
               
            
               
                 Compound 
                 ha] 
                 AMARE 
                 VIOTR 
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 320 
                 80% 
                 80% 
               
               
                   
               
               
                 inventive compound No. 3-153 
                   
                   
                   
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 320 
                 50% 
                 40% 
               
               
                   
               
               
                 compound No. 3-9, known from 
                   
                   
                   
               
               
                 WO 2008/125214 
               
               
                   
               
            
           
         
       
     
     
       
         
           
               
            
               
                   
               
               
                 Comparison table 6: Post-emergence 
               
            
           
           
               
               
               
            
               
                   
                   
                 Herbicidal 
               
               
                   
                 Dose 
                 action against 
               
               
                 Compound 
                 [g a.c./ha] 
                 SETVI 
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80 
                 100% 
               
               
                   
               
               
                 inventive compound No. 3-161 
                   
                   
               
               
                   
               
               
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 80 
                  60% 
               
               
                   
               
               
                 compound No. 3-17, known from 
                   
                   
               
               
                 WO 2008/125214