bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis and chemical reactivity of some 1,2,4‐Thiadiazolo[2,3‐a]‐pyrimidines and related compounds
Authors: Korea B. , Stanovnik B. , Tišler M. 
Published: April 2009

AbstractA novel synthetic approach for 1,2,4‐thiadiazolo[2,3‐a]pyrimidines, 1,2,4‐thiadiazolo[2,3‐c]‐pyrimidines and 1,2,4‐thiadiazolo[2,3‐b] indazoles is described. Several transformations of these heterocyclic systems are presented. 1,2,4‐Thiadiazolo[2,3‐a] pyrimidines undergo a very facile ring cleavage to give 3‐amino‐5‐carbethoxyamino‐1,2,4‐thiadiazole and similar ring opening was observed also with the isomerie [2,3‐c] system. On the other hand, 1,2,4‐thiadiazolo[2,3‐a]‐pyridines undergo under similar conditions cleavage of the thiadiazole part of the bicycle.
Sels de N‐alcoxypyridinium porteurs d'une fonction acide on ester au niveau d'un carbone α tertiaire. Synthèse et réactivite vis‐à‐vis des ions hydroxydes
Authors: Sliwa Henri , Tartar André 
Published: April 2009

AbstractAlors que le N‐oxyde de pyridine ne réagit pas directement sur l'acide α‐bromo isobutyrique ou sur son ester éthylique, les adduits correspondants sont obtenus aisément, sous forme de nitrates cristallisés 1 et 2, en effectuant la réaction en présence de nitrate d'argent en solution dans l'acétonitrile. Bien que le sel à fonction ester 2 ne soit pas sensible à la solvolyse de la liaison O‐Cα et ne puisse donner la décomposition classique selon le mode A, l'étude cinétique de son ouverture par les ions hydroxydes ne peut ětre réalisée en l'absence de réaction parasite; l'hydrolyse de la fonction ester suivie de l'ouverture de la bétaïne résultante rend alors compte d'un ordre de réaction vis à vis des ions hydroxydes supérieur à 2. Cette réaction d ouverture entre en compétition avec une décomposition carboxylogue du mode A en dioxyde de carbone, acétone et pyridine lorsque le sel à fonction acide 1 est soumis à Faction des ions hydroxydes.
Synthesis of 1‐Methyl‐3‐pyrrolin‐2‐one
Authors: Zoretic Phillip A. , Soja P. 
Published: April 2009

AbstractThe synthesis of 1‐methyl‐3‐pyrrolin‐2‐one from the oxidative‐elimination of 1‐methyl‐3‐phenylselenenyl‐2‐pyrrolidinone and from the pyrolysis of 3‐phenylsulfinyl‐2‐pyrrolidinone is reported.
Methanolysis of 2‐Phenylfuro[3,4‐d] pyrimidine‐5,7‐dione
Authors: Schuian Thomas J. 
Published: April 2009

AbstractReported is the synthesis of 2‐phenylfuro[3,4‐d]pyrimidine‐5,7‐dione which reacts with methanol to give 5‐methoxycarbonyl‐2‐phenyl‐4‐pyrimidine carboxylic acid.
Synthesis of 6‐amino‐1,2,4‐triazolo[1,5‐a]pyrazin‐4(5H)one, a bridgehead analog of guanine
Authors: Pickering Michael V. , Campbell Marie T. , Witkowski J. T. , Robins Roland K. 
Published: April 2009

AbstractThe synthesis of 6‐amino‐1,2,4‐triazolo[1,5‐a]pyrazin‐4(5H)one, an analog of guanine with a bridgehead nitrogen, is described.
The Synthesis of 2‐Carbomethoxy‐2‐carbomethoxymethyl‐2,3‐dihydro‐4(1H)quinazolinones
Authors: Beam Charles F. , Park Charles A. , Heindel Ned D. , Fives William P. 
Published: April 2009

AbstractThe treatment of anthranilhydrazides with dimethyl acetylenedicarboxylate resulted in enamines that cyclized to the six‐membered quinazolinones instead of the seven‐membered benzodiazepines.
Structure verification of (Z)‐5,6‐dihydro‐8(7H)quinolinone thiosemicarbazone by x‐ray single crystal analysis
Authors: Korp J. D. , Bernal I. , Lemke T. L. 
Published: April 2009

AbstractThe crystal structure of (Z)‐5,6‐dihydro‐8(7H)quinolinone thiosemicarbazone has been determined by X‐ray single crystal analysis in order to confirm the identity of this analog of the antineoplastic agent 2‐formylpyridine thiosemicarbazone. In the solid state, the molecules are arranged in pairs held together by intermolecular S‐N hydrogen‐bonds. There is also an extensive intramolecular N‐N hydrogen‐bonding system.
Isothiazoles X. 3‐alkoxyisothiazole derivatives
Authors: Weiler Ernest D. , Hausman Martin , Miller George A. 
Published: April 2009

AbstractHalogenation of a number of 3‐alkoxyisothiazoles, occurring exclusively in the 4‐position, followed by cyanation led to various carboxylic acid, carboxamide and amine derivatives. Subsequent dealkylation provided 4‐substituted‐4‐isothiazoIin‐3‐ones.
Potential psychotropic agents. 7‐Chloro‐9‐phenyl‐3,3‐diethyl‐3H‐pyrazolo‐[5, 1‐b]quinazolin‐10‐ium‐2‐olate and 9‐Chloro‐2,3,4,5‐tetrahydro‐1‐methyl‐3,3‐diethyl‐7‐phenyl‐1H‐benzo‐1,5,6‐triazonine‐2,4‐dione
Authors: Orzalesi Giovanni , Selleri Renato , Vittory Rodolfo Landi , Innocenti Franco , Grandolini Giuliano 
Published: April 2009

Abstract2‐Amino‐5‐chloro‐α‐phenylbenzylidene hydrazone (1) or its methyl derivative 2 or acetyl derivative 10 react with diethylmalonic esters to give the corresponding malonyl derivatives 3, 4 and 8. These esters were hydrolyzed to the acids 5 and 6. Treating 5 with dehydrating agents the mesoionic compound 7‐chloro‐9‐phenyl‐3,3‐diethyl‐3H‐pyrazolo[5,1‐b]quinazolin‐10‐ium‐2‐olate (14) was obtained, while the methyl derivative 6 afforded the desired 9‐chloro‐2,3,4,5‐tetrahydro‐1‐methyl‐3,3‐diethyl‐7‐phenyl‐1H‐benzo‐1,5,6‐triazonine‐2,4‐dione (17). Some derivatives of these compounds were also described. The structures of the new compounds were confirmed by an alternative synthesis and by mass and prnr spectral data.
Condensation of ethyl 3‐pyridylacetate with ethyl phenylpropiolate
Authors: Al‐Jallo H. N. , Al‐Azawi F. N. 
Published: April 2009

AbstractEthyl phenylpropiolate reacted with ethyl 3‐pyridylacetate in the presence of sodium ethoxide to give ethyl 3,5‐diphenyl‐4‐carbethoxy‐6‐(3‐pyridyl)salicylate (III). Different derivatives for the product were prepared and their structures were elucidated on the basis of ir and nmr spectra.
Δ3‐ and Δ4‐1,2,4‐oxadiazolin‐5‐ and 3‐ones
Authors: Boyer Joseph H. , Ellis Peter S. 
Published: April 2009

AbstractPreparations for 2,3‐diphenyl‐ and 2‐benzyI‐3‐phenyl‐Δ3‐1,2,4‐oxadiazolin‐5‐ones (3) and (4) and for 2,5‐diphenyl‐Δ4‐1,2,4‐oxadiazolin‐3‐one (7) are reported.
The configuration and solid state conformation of 3,7‐dihydroxy‐1,5‐bis(p‐bromophenyl)octahydro‐1,5‐diazocine
Authors: Peters Gary Y. , Jensen William P. , Worman James J. , Jacobson Robert A. , Nelson David A. 
Published: April 2009

AbstractThe crystal structure of 3,7‐dihydroxy‐1,5‐bis(p‐brornophenyl)octahydro‐1,5‐diazocine (4) has been determined from the three dimensional x‐ray diffraction data. This infers a similar structure for 3,7‐dihydroxy‐1,5‐diphenyloetahydro‐1,5‐diazocine (1). The molecules are in a twist crown conformation and the configuration of the hydroxyl groups on the 3,7‐positions is cis.
Synthesis of 3‐phenyl‐2H‐1,4‐benzoxazin‐2‐one. Revision of some structural assignments
Authors: Chioccara Francesco , Gala Francesco Delia , Novellino Ettore , Prota Giuseppe 
Published: April 2009

AbstractThe reported synthesis of 3‐phcnyl‐2H‐1,4‐benzoxazin‐2‐one (II) via brominution of o‐acel‐amidophenyl phcnaeyl ether (Scheme) leads in lael to the 7‐bromo‐3‐phenyl‐2H‐1,4‐benzoxazin‐2‐ol (VIII). The structure of the other synthetic intermediates is also revised and a one‐step synthesis of the lactone II is reported hy condensation of methyl phenylglyoxalale and o‐amino‐phenol.
L'ernploi du tétrafluoroborate de triéthyloxonium et ses limites, dans l'éthylation d'oxo‐2 indolinc earboxanilides et thioearboxanilides
Authors: Deberly Alain , Bourdais Jacques 
Published: April 2009

AbstractLa réaction du télrafluoroborate de Uriéthyloxonium (réaclif de Mcerwein) avec les oxo‐2 indolinc carboxanilides‐3 (4) conduit principalcment aux dérivés d'éthoxy‐2 indole, ainsi qu'á d'autres composés C‐ et O‐éthylés. Cependant, on observe également la formation de difluoro indolyloxyboranes, par réaction des anilides 4 avec le trifluorure de bore provenant de la decomposition, in situ, du réaetif de Meerwein. Ces résultats montrent certaines limites d'applications en synlhése de ce réactif.
Reaction of 3,6‐disubstituted 4‐nitropyridazine 1‐oxides with methanolic ammonia and liquid ammonia
Authors: Sakamoto T. , Van Der Plas H. C. 
Published: April 2009

AbstractReaction of 3‐chloro‐6‐methyW‐nitropyridazine 1‐oxide (5) with methanolic ammonia at 0° led to a replacement of the chlorine atom by a methoxy group as well as by an amino group. Reaction of the 3‐methoxy‐6‐methyl‐4‐nitropyridazine 1‐oxide (6) with the same reagent led to amino‐demethoxylation; this replacement reaction was very slow. Attempts to perform these reactions with liquid ammonia failed. Pmr spectroscopy of solutions of compound 6 in methanolic ammonia revealed that no σ‐adduct was present. However in liquid ammonia a 1:1 σ‐adduct at C‐5 i.e. 12b was formed. 3,6‐Dimethoxy‐4‐nitropyridazine 1‐oxide (7) gave with methanolic ammonia an amino‐demethoxylation at C‐6. No σ‐adduct could be detected by pmr spectroscopy. However, in liquid ammonia convincing pmr data were obtained showing the presence of a 1:1 σ‐adduct at C‐5.
Thieno [2,3 ‐b] pyridines and thieno [ 3,2 ‐b] pyridines by the method of gould‐jacobs
Authors: Khan Misbahul Ain , Guarçoni Antonio Elydio 
Published: April 2009

AbstractBis(2‐, and 3‐thienylammonium) hexachlorostannates were condensed with ethoxymethylene derivatives of active methylene compounds in pyridine. The resulting condensation products IVa‐IVc and Va‐Vc on heating under reflux in Dowtherm or diphenyl ether provided various 4‐hydroxythieno[2,3‐b] pyridines (Ia‐Ic) and 7‐hydroxythieno[3,2‐b]pyridines (IIa‐IIc). The compound Ic on further transformations gave yet other derivatives If‐Ik.
Imidazo [4,5‐c] ‐ and [4,5‐6] pyridines
Authors: Denzel Theodor , Höhn Hans 
Published: April 2009

AbstractThe synthesis of novel imidazo[4,5‐c]pyridines 11‐13 and imidazo[4,5‐b]pyridines 18‐20 is described using 2 as the starting material. The synthesis is generally applicable for the introduction of a wide variety of substituents.
The synthesis and reactivity of some 2‐amino‐5‐bromo‐],1,3,4‐thiadiazoles and the corresponding Δ2‐1,3,4‐thiadiazolines
Authors: Werber Giuseppe , Buccheri Francesco , Gentile Manlio 
Published: April 2009

AbstractThe synthesis of some 2‐amino‐5‐bromo‐1,3,4‐thiadiazoles is reported; these substrates are found to behave as ambidenl nucleophiles in alkylation, aeylation and nitrosation reactions, giving thiadiazoliens along with thiadiazole derivatives. This finding suggests amine‐imine tautomerism between these compounds and the corresponding Δ2‐1,3,4‐thiadiazolines.
Isomeric maleic anhydride adducts of phthalazine and pyridazine and their partial stereochemistry
Authors: Hocking M. B. 
Published: April 2009

AbstractThe addition of maleic anhydride to phthalazine is confirmed to form a five‐membered pyrrolidino ring fusion to phthalazine VI, rather than a pyridophthalazine II, by means of synthetic and degradative experiments, and proton and carbon‐13 nmr. Two of probable three isomers obtained have been isolated and the stereochemistry partially established. Comparison of the data obtained for this adduct with the data obtained for the adduct of maleic anhydride with pyridazine demonstrates that it too possesses the pyrrolidino ring fusion. Electron impact fragmentations of the two adducts are compared and are related to the breakdown of 1H,2H‐pyridazinone.
Recherches sur le benzofuranne. LX. Orientation de la dégradation alcaline des aroyl‐3 éthyl‐2 benzofurannes, selon la nature de leur groupe aroyle
Authors: Astoin Jacques , Demerseman Pierre , Riveron André , Royer René 
Published: April 2009

AbstractFar dégradation alcaline suivie de recyclisation acido‐catalysée, les aroyl‐3 éthyl‐2 benzofurannes donnent des aryl‐2 benzofurannes, avec des rendements qui dépendent notamment de 1′effet stérique des substituants du groupe aroyle.Ce precédé convient particuliérement pour la synthése de benzofurannes substitutés en 2 par un phényle encombré.
Optishift PMR spectroscopic studies on some quinoxaline amino esters and dipeptides
Authors: El‐Abadelah Mustafa M. , Sabri Salim S. , Tabba Hani D. , Duddeck Helmut 
Published: April 2009

AbstractOptishift pmr spectral measurements on a series of N‐(2‐quinoxaloyl)α‐amino esters and the C3‐CH3 analogues indicate that their L‐isomers are optically pure. Such measurements also show that the Eu atom in Eu(tfc)3 preferentially complexes with the amide carbonyl. Similar optishift pmr studies on model quinoxaline‐dipeptide esters reveal that the amino‐terminal α‐amino acid suffers appreciable racemization during the coupling process with triphenylphosphite‐pyridine, whereas no detectable racemization is observed with diphenylphosphoryl azide. A Bystrov's model is suggested for the quinoxaline‐dipeptide‐Eu complexes studied. The benzylic protons of phenylalanine and the isopropyl methyls in their quinoxaline derivatives show signal splitting due to diastereotopy in the presence of Eu(tfc)3.
2‐Aminothiazole derivatives. I. Mass spectra of 2‐acetylacetamidothiazoles and N‐(2‐thiazolyl)‐β‐(2′‐thiazolylamino)crotonamides
Authors: Saint‐Ruf G. , Silou Th. 
Published: April 2009

Abstract2‐Acetylacetamidothiazoles (2) and N‐(2‐thiazolyl)‐β‐(2′‐thiazolylamino)crotonamides (3) break down in a well‐defined manner upon electron impact. In either of the two cases, the fragmentation pattern involves hydrogen transfer, similar to the McLafferty rearrangement. The principal ions formed are characterised and the most plausible mechanism of their formation is discussed.
Heteroaromatic boron compounds. XV. Deuteriodeprotonation in some borazarothienopyridines and thienopyridines
Authors: Gronowitz Salo , Roos Curt , Sandberg Elina , Clementi Sergio 
Published: April 2009

AbstractDeuteriodeprotonation of some substituted 4,5‐borazarothieno[2,3‐c]pyridines (I) and 7,6‐borazarothieno[3,2‐c]pyridines (II) has been studied by the nmr technique. Exchange occurred predominantly in the 3‐position, and the effect of methyl substitution on rate is discussed. The rates of exchange in some derivatives of I and II were compared with those of the isoelectronic thieno[2,3‐c]pyridines (III) and thieno[3,2‐c]pyridines (IV). Similar rates were obtained, confirming the aromatic nature of I and II. The deuteriodeprotonation of 4‐methyl‐4,5‐borazaro‐thieno[2,3‐c]pyridine (Ie), 7‐methyl‐7,6‐borazarothieno[3,2‐c]pyridine (IIe), 4‐methylthieno‐[2,3‐c]pyridine (IIIe), and 7‐methylthieno[3,2‐c]pyridine (IVe) were measured at different concentrations of deuteriosulfuric acid and different temperatures, showing that the protonated heterocycles are substrates in the deuteriodeprotonation reaction. Standard rates at p0 H and 100° were calculated for these systems.
An investigation of oxidative animation of 2‐methyl‐1,4‐benzoquinone with pyrrolidine
Authors: Shaikh Yunus A. 
Published: April 2009

AbstractOxidative amination of 2‐methyl‐1,4‐benzoquinone with pyrrolidine yielded 2‐methyl‐6‐pyrrolidino‐1,4‐benzoquinone as the major product along with 2‐methyl‐5‐pyrrolidino‐1,4‐benzoquinone formed as the minor product. No detectable amount of 2‐methyl‐3,6‐bis‐(pyrrolidino)‐1,4‐benzoquinone was observed.
Pyrazolones and quinoxalines from 4‐phenyl‐2,3‐dioxobutyro‐1,4‐lactone
Authors: Mokhtar H. M. , El‐Shafei Z. M. , El Khadem H. S. , Swartz D. L. 
Published: April 2009

Abstract4‐Phenyl‐2,3‐dioxobutyro‐1,4‐lactone (1) gave with phenylhydrazine and ils p‐Cl, p‐Br, p‐I and p‐NO2 derivatives, bishydrazones which were eyclized to 1‐aryl‐3‐(α‐hydroxybenzyl)‐4,5‐dione‐4‐arylhydrazones. With o‐phenylene diamine, compound 1 gave either a Schiff base or a substituted quinoxaline, depending upon the ratio of the reactants.
Synthesis of a pyrano[2,3‐b] pyridine with vinylogous hydroxamic acid structures
Authors: Löwe Werner 
Published: April 2009

AbstractA new, two step synthesis of a pyrano[2,3‐b]pyridine derivative 5 is described. Dehydro‐acetic acid and N,N‐dimethylformamide dimethylacetal was condensed to form 2. Compound 2 was converted into 5 by reaction with hydroxylamine which opens the lactone ring.
Evidence for an indirect halogen exchange in the reaction of trans‐ 2,3‐dibromo‐2,3‐dihydrobenzofuran with chloride ions
Authors: Baciocchi Enrico , Clementi Sergio , Ruzziconi Renzo , Sebastiani Giovanni V. 
Published: April 2009

AbstractTreatment of the title compound with chloride ions in acetonitrile leads mainly to the formation of trans‐2,3‐dichloro‐2,3‐dihydrobenzofuran. Since a nucleophilic displacement of bromide anion by chloride anion can be excluded, a mechanism involving the equilibrium 2Cl− + Br2 ⇋ 2Br− + Cl2 is suggested.
Photodimerization of 3‐methyl‐4‐nitro‐5‐styrylisoxazole in the solid state
Authors: Donati D. , Fiorenza M. , Moschi E. , Sarti‐Fantoni P. 
Published: April 2009

AbstractThe photoreactivity of 3‐methyl‐4‐nitro‐5‐styrylisoxazole in the solid state was studied and the centrosymmetric product identified.
Chloration et S‐oxydation du benzo[b]thiophène par l'hypochlorite de tertiobutyle. Mécanisme de la réaction
Authors: Geneste Patrick , Olivé Jean‐Louis , Ung Sak Neng 
Published: April 2009

AbstractDans la réaction avec le benzothiophène, l'hypochlorite de tertiobutyle intervient comme réactif d'oxydation et de chloration: c'est en effet une source d'acide hypochloreux et de chlore. L'é'tape primaire de la réaction est une S‐oxydation conduisant au sulfoxyde du benzothiophène qui réagit trAès rapidement avec le chlore formé pour donner des composés d'addition. Le passage intermédiare par le benzothiophène 1‐oxyde a eté mis èn evidence par la technique du flux stoppé en spectroscopic uv. J. Heterocyclic Chem., 14, 953 (1977).
The synthesis of l‐alkyl‐2‐benzoyl‐4‐methylazetidine. Configurational and conformational studies
Authors: Kulkarni Shrikant B. , Cromwell Norman H. 
Published: April 2009

Abstractα,γ‐Dibromovalerophenone (3) reacted with primary amines to give a number of l‐alkyl‐2‐benzoyl‐4‐methylazetidines (4) in good yield. The results of the base catalyzed reactions performed on these new carboazetidines imply that the cis isomer is of greater thermodynamic stability. Furthermore, base catalyzed deuterium exchange studies suggest this to be the case. J. Heterocyclic Chem., 14, 981 (1977)
Studies on the chemistry of 2,3,5,6‐tetrahydro‐6‐phenylimidazo[2,l‐b]‐thiazole. III. . Reaction with isocyanates and isothiocyanates
Authors: Bigg D. C. H. , Faull A. W. , Purvis S. R. 
Published: April 2009

Abstract2,3,5,6‐Tetrahydro‐b‐phenylimidazo[2,l‐b‐]thiazole reacts with aryl isothiocyanates to give dipolar 1:1 adducts. The adducts are relatively unstable and, in solution, exist in equilibrium with starting materials. The reaction with aryl and alkyl isocyanates, however, leads to cyclic 2:1 adducts, while sulphonyl and acyl isocyanates give stable dipolar 1:1 adducts. J. Chem. Soc., 14, 989 (1977)
Thermolysis of the reaction products from 2‐pyridylacetohydrazide and nitrous acid
Authors: Iwao Masatomo , Kuraishi Tsukasa 
Published: April 2009

Abstract2,3‐Dihydroimidazo[1,5‐α]pyridin‐3‐one (IV) was obtained by thermolysis of 2‐pyridylacetyl azide (II) which was prepared from 2‐pyridylacetohydrazide (I) on treatment with an equivalent mole of nitrous acid. Treatment of I with excess nitrous acid yielded α‐oximino‐α:‐(2‐pyridyl)‐acetylazide (V). Thermal decomposition of V gave 3‐(2‐pyridyl)‐1,2,4‐4H‐oxadiazolin‐5‐one (VII). 2‐Cyanopyridine (IX) was obtained from V by the action of alkali. 2,3‐Dihydroimidazo‐[1,5‐α ]pyridin‐3‐one (IV) was rearranged to VII upon treatment with nitrous acid. J. Chem. Soc., 14, 993 (1977)
A facile synthesis of 2‐substituted‐4‐(substituted)phenyl‐Δ2‐1,3,4‐oxadiazolin‐5‐ones
Authors: Pilgram Kurt , Skiles Richard D. 
Published: April 2009

AbstractThe title compounds, 3, are formed at ambient temperature from 4,4‐dimethyl‐2‐(substituted)‐phenylsemicarbazides (1) and carboxylic acid chlorides in the presence of triethylamine. 2‐Dimethylamino‐4‐(substiluted)phenyl‐Δ2‐1,3,4‐oxadiazolin‐5‐ones are formed from 1 and dialkyl‐carbamoyl chlorides at elevated temperature (about 15° ). Acylation of 1 with carboxylic acid anhydrides, also at elevated temperature, is accompanied by loss of dimethylamine from the intermediate l‐acyl‐4,4‐dimethyl‐2‐(substituted)phenylsemicarbazides, 2, to give 3.
Synthesis of 5H[l]benzopyrano[3,4‐b]pyridin‐5‐one and its derivatives
Authors: Khan Misbahul Ain , Gemal Andre Luis 
Published: April 2009

Abstract3‐Aminocoumarin undergoes the Skraup reaction to give a new ring system, 5H[l]benzo‐pyrano[3,4‐b]pyridin‐5‐one (IVa). When 3‐aminocoumarin was condensed with the ethoxy methylene derivatives of active methylene compounds, ethyl acetoacetate, and dimethyl acetylenedicarboxylate, the intermediates Vla‐VIf were formed which on thermal cyclizations afforded other derivatives of 5H[l ]benzopyrano[3,4‐b]pyridin‐5‐one (IVb‐IVf). The nitration of IVa gave IVg.
Recherches en série diazépine‐1,4 et triazépine‐1,2,4. X. Réductions et méthylations de pyrazolo[3,4‐b]diazépines‐1,4
Authors: Affane‐Nguéma J.‐P. , Lavergne J.‐P. , Viallefont Ph. 
Published: April 2009

AbstractLes réductions et méthylations de pyrazolo[3,4‐b]diazepines‐1,4, selon différentes méthodes, ont été réalisées.Selon les agents de réduction, il a été possible de réduire sAélectivement une double liaison C=N, le groupe carbonyle ou d'effectuer la rAéduction totale des cycles diazépinones, de réduire partiellement ou totalement les insaturations des (6H)pyrazolodiazépines.La méthylation a pu ětre obtenue sur l'atome d'azote amidique, sur Patome d'oxygène de la měme fonction, dans quelques cas sur l'atome de carbone C6 des pyrazolodiazépinones et enfin sur la position 4 des tétrahydro pyrazolodiazépinones.
New syntheses of condensed heterocycles from isoxazole derivatives. V. Pyrrolo[3,4‐b ]pyridin‐4‐ones
Authors: Dattolo G. , Aiello E. , Plescia S. , Cirrincione G. , Daidone G. 
Published: April 2009

AbstractHydrogenolysis with Raney‐Nickel or iron powder in acetic acid of 2,5‐diphenyl‐4‐nitro‐3‐(3,5‐R,R‐4‐isoxazolyl)pyrrolyl ketones, prepared by the Grignard reaction of 2,5‐diphenylpyrrole and 3,5‐R,R‐4‐isoxazolecarboxilic acid chlorides followed by nitration, afforded directly the desired 6H‐pyrrolo[3,4‐b ]pyridin‐4‐ones.
Synthesis of alkyl indole derivatives
Authors: Shaikh Yunus A. 
Published: April 2009

AbstractCondensation of arylamines with α‐halogenoketone afforded the intermediate anilino‐ketones which on direct cyclization furnished the corresponding alkylindoles. Synthesis of 2,3,5‐trimethyl‐4,7‐dimethoxyindole (5a) and 2,3,6‐trimethyl‐7‐methoxyindole (5b) is described. Earlier (1) synthesis of 2,3‐dimethyl‐4,7‐dimethoxyindole and 1,2,3‐trimethyl‐4,7‐dimethoxy‐indole is reported.
Pyrimido[5,4‐b]quinolines. III. Synthesis of 10‐alkyl‐substituted 10‐deazaalloxazines
Authors: Chu C. K. , Bardos T. J. 
Published: April 2009

AbstractA general method for the synthesis of 10‐alkyl‐substituted 10‐deazaalloxazines (VIII) and the related chemistry are described. 4‐Alkyl‐substituted 3‐aminoquinolines (IV) were reacted with benzoyl chloride and potassium cyanide in methylene chloride‐water mixture to obtain Reissert compounds (V) which were hydrolyzed with a mixture of hydrobromic acid and acetic acid, and subsequently with 20% potassium hydroxide to give the corresponding 3‐aminoquinaldic acids (VII). Cyclization with urea gave the 10‐deazaalloxazines (VIII). Oxidation, hydroxylation and alkylation reactions of the 10‐methyl derivatives (VIIIa,b) and of their quinaldic acid precursors are also reported.
Chemistry of the phenoxathiins i. Synthesis of 1‐azaphenoxathiin analogs as potential new CNS depressant agents
Authors: Martin G. E. , Turley J. C. , Williams L. , Steenberg M. L. , Buckley J. P. 
Published: April 2009

AbstractThe condensation of the disodium salt of 2‐mercapto‐3‐pyridinol with various ortho‐nitrohalo‐benzenes to yield a group of previously unreported 1‐azaphenoxathiins is described. The synthetic pathway and the substituent location on the products is unequivocably demonstrated by Fourier Transform1 3 C‐nmr. Preliminary pharmacologic evaluation of the title compounds as potential CNS depressant agents is also reported.