bluuebunny/crossref_metadata_2025_split huggingface dataset:
Cycloaddition dipolaire‐1,3 des arylnitriloxydes sur les dihydro‐1,2 quinoleines n‐substituees
Authors: Soufiaoui M. , Jazouli H. 
Published: March 2009

AbstractLa réaction de cycloaddition dipolaire‐1,3 des arylnitriloxydes sur la dihydro‐1,2 quinoléine donne deux adduits si l'atome d'azote du dipolarophile porte un groupement benzoyle. Par contre la réaction ne fournit qu'un seul adduit si le groupement est un benzyle. La structure des cycloadduits a été établie par voies spectroscopique et chimique.The 1.3‐depolar cycloaddition reacton of arylnitrile oxides on 1,2‐dihydroquinolines gives two adducts if the nitrogen atom of the dipolarphile carries a benzoyl group. The structure of the cycloadducts has been established by spectoscopic and chemical methods.
Novel dyestuffs containing dicyanomethylidene groups
Authors: Katritzky Alan R. , Fan Wei‐Qiang , Liang De‐Sheng , Li Qiao‐Ling 
Published: March 2009

AbstractSeveral series of novel compounds have been prepared containing dicyanomethylidene groups including 1‐alkyl‐3‐dicyanomethylideneindol‐2‐ones and 6,6‐dicyanofulvenes. Their visible absorption properties are recorded and discussed.
Reinvestigation of a 5H‐dibenzo[d,h][1,3,6]triazonine synthesis
Authors: Peet Norton P. , Sunder Shyam , Barbuch Robert J. , Whalon Michael R. , Huber Edward W. , Huffman John C. 
Published: March 2009

AbstractTreatment of 5‐chloro‐2‐aminobenzophenone (1) witho‐phenylenediamine, sodium acetate, and acetic acid gave 2‐(acetyl)amino‐5‐chlorobenzophenone (5) rather thanN‐[(2‐amino‐5‐chlorophenyl)phenylmethylene]‐1,2‐benzenediamine (3), as reported by Kulkarniet al, [1]. Authentic3was prepared and treated with chloroacetic acid and polyphosphoric acid (PPA) to give1, recovered3, 2,8‐dichloro‐6,12‐diphenyldibenzo[b,f][1,5]diazocine (9) and 2‐chloro‐6‐(chloromethyl)‐13‐phenyl‐5H‐dibenzo[d,h][1,3,6]triazonine (10). Treatment of5with PPA, with or without chloroacetic acid, gave [5‐chloro‐2‐[(6‐chloro‐4‐phenyl‐2‐quinolinyl)amino]phenyl]phenylmethanone (11) as the sole product in 90% yield. Treatment of other benzophenones, acetophenones, and anilines with sodium acetate and acetic acid provided acetanilides in 78‐96% yield, with the exception of 2′‐aminoacetophenone (20), which gave a quantitative yield of 2‐[((2‐acetyl)phenyl)amino]‐4‐methylquinoline (21). The mechanism of acetanilide formation with sodium acetate and acetic acid is discussed. The structure of21was established using high resolution1H nmr techniques. Attempts to prepare an authentic sample of21from 2‐chlorolepidine (26) and (20) gave 4‐methyl‐N‐[2‐(4‐methyl‐2‐quinolinyl)phenyl]‐2‐quinolinamine (29) as the major product.
Cycloaddition reactions of 2,3‐dihydro‐1H‐1,4‐diazepines with nitrile oxides and imines. Synthesis of bis[1,2,4]oxadiazolo‐and bis[1,2,4]triazolo[1,4]diazepine derivatives
Authors: Aversa Maria C. , Bonaccorsi Paola , Giannetto Placido , Leigh David A. 
Published: March 2009

AbstractNew heterotricyclic systems, 6,10a,11,11a‐tetrahydro‐5H‐bis[1,2,4]oxadiazolo[4,5‐d:5′,4′‐g][1,4]diazepines 6,7,9‐11 and 5,6,10,10a,11,11a‐hexahydro‐1H‐bis[1,2,4]triazolo[4,3‐d:3′,4′‐g][1,4]diazepines 8,12 have been obtained by double site‐ and regie‐specific 1,3‐dipolar cycloaddition of mesitylnitrile oxide (1) or diphenylnitrile imine (2) to 5,7‐disubstituted 2,3‐dihydro‐1H‐1,4‐diazepines 3‐5. The structure of the synthesized bis‐adducts 6‐12 shows that the hetero double bonds are much more reactive than the olefinic ones in the dipolarophiles under study. No evidence for the formation of mono‐adducts was obtained.
New quinoxaline and pyrimido[4,5‐b]quinoxaline derivatives. Potential antihypertensive and blood platelet antiaggregating agents
Authors: Monge A. , Palop J. A. , Urbasos I. , Fernández‐Alvarez E. 
Published: March 2009

AbstractStarting with 3‐amino‐2‐quinoxalinecarbonitrile 1,4‐dioxide 1, a new series of quinoxaline derivatives 2‐12 was synthetized through chemical modification of the 3‐amino group, the 2‐cyano group and selective mono‐deoxygenation of the 1‐oxide or 4‐oxide groups. On the other hand, two 2,4‐diaminopyrimido[4,5‐b]quinoxa‐line derivatives 13, 14 were obtained condensing 3‐amino‐2‐quinoxaline carbonitriles with quanidine. Some of the new compounds were studied as inhibitors of blood platelet aggregation as well as antihypertensive agents.
3′‐(1,2,3‐Triazol‐1‐yl)‐2′,3′‐dideoxythymidine and 3′‐(1,2,3‐triazol‐1‐yl)‐2′,3′‐dideoxyuridine
Authors: Wigerinck Piet , Van Aerschot Arthur , Claes Paul , Balzarini Jan , De Clercq Erik , Herdewijn Piet 
Published: March 2009

AbstractCycloaddition of different acetylenic compounds on the azido function of 3′‐azido‐2′,3′‐dideoxythymidine and 3′‐azido‐2′,3′‐dideoxyuridine afforded products with a 1,2,3‐triazol‐1‐yl substituent in the 3′‐position. In contrast with the parent compounds, these triazolyl derivatives had no appreciable activity against human immunodeficiency virus (HIV‐1).
Alkylation of tetraazapentalene derivatives having a hypervalent sulfur or selenium using alkyl iodide
Authors: Matsumura Noboru , Tomura Masaaki , Inoue Hiroo 
Published: March 2009

AbstractAlkylation of 2,3,4a,7a‐tetraazapentalene derivatives having a hypervalent sulfur or selenium using alkyl iodide in benzene under reflux afforded the S‐monoalkylated tetraazapentalene derivatives 3 and 4 in good yields.
The cycloaddition of heterocumulenes to oxetanes in the presence of catalytic amounts of tetraphenylstibonium iodide
Authors: Fujiwara Masahiro , Baba Akio , Matsuda Haruo 
Published: March 2009

AbstractThe cycloadditions of carbon dioxide, isocyanates and carbodiimides to oxetanes proceeded in the presence of catalytic amounts of tetraphenylstibonium iodide (1) under mild conditions, affording the corresponding six‐membered heterocycles; 1,3‐dioxan‐2‐ones, 1,3‐oxazin‐2‐ones and 1,3‐oxazin‐2‐imines in good yields, respectively. Moreover, the cycloaddition of 2‐phenyloxetane proceeded via predominant ring‐cleavage at substituted site.
New heterocyclic structures. [1,3]Thiazino[3,2‐a]purine and [1,2,3]triazolo[4,5‐d][1,3]thiazino[3,2‐a]pyrimidine
Authors: Pecorari Piergiorgio , Rinaldi Marcella , Costi Maria Paola 
Published: March 2009

AbstractDerivatives of two new molecular structures, namely, [1,3]thiazino[3,2‐a]purine and [1,2,3]triazolo[4,5‐d]‐[1,3]thiazino[3,2‐a]pyrimidine, were synthesized together with other heterocyclic compounds. Retrosynthetic analysis of their molecular skeletons suggested a simple way of obtaining 3,4‐dihydro‐7,8‐diamino‐2H,6H‐pyrimido[2,1‐b][1,3]thiazin‐6‐one, which is a useful intermediate for their synthesis. This intermediate and the thiazole homologue were obtained directly by reaction of 5,6‐diamino‐2,3‐dihydro‐2‐thioxo‐4(lH)‐pyrimidi‐none with 1,3‐ or 1,2‐dibromoalkane, respectively.
Acid‐catalyzed reactions of 3‐(hydroxymethyl)‐ and 3‐(1‐hydroxyethyl)pyrazolo[1,5‐a]pyridines
Authors: Miki Yasuyoshi , Nakamura Noriko , Hachiken Hiroko , Takemura Shoji 
Published: March 2009

AbstractTreatment of 3‐(hydroxymethyl)pyrazolo[1,5‐a]pyridines with trifluoroacetic acid in refluxing dichloro‐methane led to the formation of bis(pyrazolo[1,5‐a]pyrid‐3‐yl)methanes or bis[(pyrazolo[1,5‐a]pyrid‐3‐yl)]‐methyl ethers depending upon the concentration of trifluoroacetic acid. In contrast, similar treatment of 3‐(1‐hydroxyethyl)pyrazolo[1,5‐a]pyridines gave a mixture of 3‐vinylpyrazolo[1,5‐a]pyridines and 1,3‐bis(pyrazolo‐[1,5‐a]pyrid‐3‐yl)‐1‐butenes.
Synthesis of bridged heteroaromatic compounds as reference standards for coal degradation products
Authors: Luo Jiann‐Kuan , Takahashi Kazufumi , Mckenney J. Dew , Castle Raymond N. , Lee Milton L. 
Published: March 2009

AbstractThe synthesis of 2‐naphthyl 2′‐dibenzothienyl ether, 1‐(1′‐naphthyl)‐2‐(4″‐acridinyl)ethane and a series of naphthylethyldibenzothiophenes is reported.
Studies on the chemistry of 5‐propynyloxy‐ and 5‐propynylthiopyrimidines: New syntheses of furo‐ and thieno[3,2‐d]pyrimidines
Authors: Spada Marianne R. , Klein Robert S. , Otter Brian A. 
Published: March 2009

AbstractThe utility of certain 5‐alkynyloxy‐, 5‐alkynylthio, and 5‐alkynylsulfinyl‐pyrimidines as precursors of 7‐substituted furo[3,2‐d]‐ and thieno[3,2‐d]pyrimidines has been examined. When treated with sodium methoxide in warm methyl sulfoxide, 1,3‐dimethyl‐5‐(2‐propynyloxy)uracil (6) cyclizes to afford 1,3,7‐tri‐methylfuro[3,2‐d]pyrimidine‐2,4‐(1H,3H)‐dione (12) in 52% yield, possibly via the allenic ether 9 (R = H). The corresponding 5‐(2‐butynyloxy)pyrimidine (7), obtained in good yield by treating 6 with methyl iodide and sodium hydride in methyl sulfoxide, fails to undergo an analogous cyclization. However, compound 7 does undergo a normal alkynyl Claisen rearrangement and cyclization when heated at 130°, giving the 8‐methylpyrano[3,2‐d]pyrimidine 8 in methyl sulfoxide and the 6,7‐dimethylfuro[3,2‐d]pyrimidme 11 in dimethylformamide. The 5‐(2‐propynylthio)pyrimidine 15 affords the allene 19 and the 1‐propyne 22 when treated with various bases, but none of the 7‐methylthieno[3,2‐d]pyrimidine 16. At 145° in methyl sulfoxide, 15 undergoes a thio‐Claisen rearrangement process to afford the 6‐methylthieno[3,2‐d]pyrimidine 17 together with substantial amounts of a product 20 that bears a 7‐thiomethoxymethyl substituent derived from the solvent. Heating the 5‐(2‐propynylsulfinyl)pyriniidine 23 at 105° in methyl sulfoxide, followed by acidification of the reaction mixture, affords 1,3‐dimethyl‐7‐formylthieno[3,2‐d]pyrimidine‐2,4‐(1H,3H)‐dione (29) in 47% yield. Deuterium labelling studies established that the aldehyde proton of 29 is derived from the 3′‐proton of 23. This finding is consistent with a mechanism that involves sequential [2,3] and [3,3] sigma‐tropic rearrangements, and the intermediacy of a dihydrothieno[3,2‐d]pyrimidine such as compound 30.
Synthesis of vinca alkaloids and related compounds.XLVI.. Formation of a new ring system
Authors: Dancsó András , Kajtár‐Peredy Mária , Szántay Csaba 
Published: March 2009

AbstractIn the Pictet‐Spengler reaction of indole‐3‐propanamine1and diethyl‐(2‐formyl‐cyclopropane‐1,1‐dicar‐boxylate)2the formation of ethyl (1a,2,4,5,6,11,11b,11c‐octahydro‐2‐oxo‐1H‐cycloprop[3′,4′]pyrrolo[1,2′:1,2]‐azepino[3,4‐b]indole‐1a‐carboxylates)3and4was observed. Compounds3and4represent a new ring system.
Oxidation of heterocyclic nitrogen ylids to nitro heterocycles. Comparison of dimethyldioxirane with peracids
Authors: Coburn Michael D. 
Published: March 2009

AbstractOxidation of 3‐amino‐4‐(4‐chlorophenyl)furazan (1) and its phosphine imine derivative, 3‐(4‐chlorophenyl)‐4‐trioctylphosphiniminofurazan (3), with dimethyldioxirane (DMD) gave 3‐(4‐chlorophenyl)‐4‐nitrofurazan (4) as the exclusive product. However, the sulfilimine derivative, 3‐(4‐chlorophenyl)‐4‐dimethylsulfiliminofurazan (2), was converted by DMD to the sulfoximine, 3‐(4‐chlorophenyl)‐4‐dimethylsulfoximinofurazan (6). These results contrast dramatically with the oxidations of these compounds with peracids.
Formation of oxadiazolo[4,5‐a]indolines via addition reactions of cycloalkano[b]indoles with nitrile oxides. Crystal structure of an adduct
Authors: Coutouli‐Argyropoulou E. , Malamidou‐Xenikaki E. , Mentzafos D. , Terzis A. 
Published: March 2009

AbstractReactions of stable nitrile oxides with cycloalkano[b]indoles gave as main product adducts 3 containing the oxadiazolo[4,5‐a]indoline ring system. The structure elucidation of the isolated adducts was based on their spectral data, chemical behaviour and in one case the structure was confirmed by crystallographic X‐ray analysis. The mechanism of the reaction is also discussed.
Synthesis of quinoline derivatives using ketene dithioacetals
Authors: Tominaga Yoshinori , Michioka Takeharu , Moriyama Kohu , Hosomi Akira 
Published: March 2009

AbstractMethyl 3‐(N‐arylamino)‐2‐cyano‐3‐methylthioacrylates 3a‐h, which are readily prepared by the reaction of the ketene dithioacetal, methyl 2‐cyano‐3,3‐bis(methylthio)acrylate (1) with arylamines, was heated at reflux in diphenyl ether to give the corresponding 2‐methylthio‐4‐hydroxyquinoline‐3‐carbonitriles 4a‐h in 14–77% yields. The reaction of 1 with excess aryl amines in diphenyl ether at reflux gave also the corresponding 2‐arylamino‐4‐hydroxyquinoline‐3‐carbonitriles 6a‐d. The 2‐methylthioquinoline‐3‐carbonitriles 4a‐h, thus obtained, are useful intermediates for the synthesis of various quinoline derivatives.
Synthesis of large macrocyclic tetraaza compounds with a methylene backbone: Cyclo[‐NH‐ (CH2)n‐]4, (n = 6, 7, 8, 9 and 10). The formation of 28‐, 32‐, 36‐, 40‐ and 44‐membered rings
Authors: Tomohiro Takenori , Uoto Kouichi , Okuno Hiroaki (Yohmei) 
Published: March 2009

AbstractA series of macrocyclic tetraamines with 28‐, 32‐, 36‐, 40‐ and 44‐membered rings have been efficiently prepared from the corresponding ditosylamide and monobromoalcohol derivatives in 6 steps via a double condensation reaction. Overall yields were: 41, 41, 46, 29, and 33%, respectively, for 1,8,15,22‐tetraazacyclooctacontane (11a), 1,9,17,25‐tetraazacyclodotriacontane (11b), 1,10,19,28‐tetraazacyclohexatriacontane (11c), 1,11,21,31‐tetraazacyclotetracontane (11d) and 1,12,23,34‐tetraazacyclotetratetracontane (11e).
Synthesis of 3‐aminopyrazolo[3,4‐d]pyrimidine derivatives using N‐bis(methylthio)methylene‐p‐toluenesulfonamide
Authors: Tominaga Yoshinori , Hara Mayumi , Honkawa Harumasa , Hosomi Akira 
Published: March 2009

AbstractN‐Bis(methylthio)methylene‐p‐toluenesulfonamide (1) reacted with active methylene compounds such as malononitrile (2a) and, cyanoacetamide (2b) to give the corresponding 3‐methylthio‐3‐p‐toluenesulfonylami‐nopropenenitrile derivatives 3a,b which were found to be convenient starting materials for the synthesis of 3,5‐diaminopyrazole derivatives. Reaction of 3a and 3b with hydrazines gave the corresponding 3,5‐diaminopyrazoles 4a‐e, key intermediates for the synthesis of 3‐aminopyrazolo[3,4‐d]pyrimidine derivatives 5a‐d.
On triazoles. XXI. Synthesis of 1,2,4‐triazolyldithiocarbonates
Authors: Pongó László , Reiter József , Barkóczy József , Sohár Pál , Pallagi István 
Published: March 2009

AbstractThe reaction of 5‐amino‐1,2,4‐triazoles 1 with carbon disulfide and alkylating agents in basic condition to yield alkyl, aralkyl and aryl (5‐amino‐3‐Q‐1,2,4‐triazol‐1‐yl)dithiocarbonates 2 and alkyl (3‐Q‐1,2,4‐triazol‐5‐yl‐amino)dithiocarbonates 3 was studied. The isomeric and tautomeric structure of derivatives obtained was proved with the help of their uv, pmr and cmr spectra using model compounds prepared for this purpose. The results obtained enabled us to correct some confusion in the literature.
Diheterocyclic compounds from dithiocarbamates and derivatives thereof. IV. 3,3′‐arylenebis‐(4‐oxo‐2‐thioxo‐1,2,3,4‐tetrahydroquinazolines)
Authors: Garín Javier , Meléndez Enrique , Merchán Francisco L. , Merino Pedro , Orduna Jesús , Tejero Tomás 
Published: March 2009

AbstractThe title compounds 3 were synthesized in one step from bisdithiocarbamates 2, and their structures were confirmed by two independent syntheses. Alkylation and hydrolysis of 3 gives 3,3′‐arylenebis(2,4‐dioxo‐1,2,3,4‐tetrahydroquinazolines) 8.
Réactivité des esters de la carboxyméthylène‐1 hydroxy‐4 méthyl‐6 pyridone‐2 vis‐à‐vis des aldéhydes aromatiques
Authors: Kherfi Houria‐Nacera , Hamdi Maâmar , Spéziale Vincent 
Published: March 2009

AbstractUne nouvelle réaction de condensation d'aldéhydes aromatiques sur des pyridones‐2 a été examinée. La carboxyméthylène‐1 hydroxy‐4 méthyl‐6 pyridone‐2 1 et les esters méthylique et éthylique correspondants 2 et 3 ont permis de synthétiser des arylméthanes par réaction entre une molécule d'aldéhyde et deux molécules de pyridone. l'étude spectroscopique des dérivés obtenus a été réalisée et un mécanisme réactionnel pour leur formation a été proposé.
Synthesis of 1,2,3‐thiadiazole‐5‐carbaldehydes and their conversion into 6aδ4‐Thia‐1,2,5,6‐tetraazapentalenes
Authors: L'Abbé Gerrit , Frederix Ann 
Published: March 2009

AbstractA convenient method for the synthesis of the virtually unknown 1,2,3‐thiadiazole‐5‐carbaldehydes consists in monobromination of the 5‐methyl derivatives, followed by treatment with sodium azide and decomposition in concentrated sulfuric acid (6 → 7 → 9 → 10). These compounds can be transformed via methylation of the corresponding hydrazones 12 into 6aδ4‐thia‐1,2,5,6‐tetraazapentalenes 13.
Palladium‐catalyzed synthesis of isocoumarin and 1‐isoquinolinone derivatives
Authors: Izumi Taeko , Nishimoto Yasuhiro , Kohei Kunihiro , Kasahara Akira 
Published: March 2009

AbstractIn the presence of copper(I) chloride, the palladium catalyzed oxidation of methyl 2‐ethenylbenzoates and 2‐ethenylbenzamides have been studied. This reaction was used to form isocoumarins and 1‐isoquinolinones.
Reaction of electron rich heterocycles with electrophiles. Formylation of indoles via thiomethylation
Authors: Akgün Eyup , Tunali Mustafa 
Published: March 2009

AbstractThe formylation of indoles 1 by dithiocarbenium‐ions 2 is discussed. The reaction proceeds to thioacetals 4 under mild conditions. Longer reaction times yield bisindolylmonomethylcyanines 5–6. Generally, the reaction is inhibited by the presence of electron‐withdrawing groups at the pyrrol nucleus of indole 1, e.g. an acetyl group.
2H‐1,2,4‐benzothiadiazine 1,1‐dioxides 2. A condensation of 2‐aminobenzenesulfonamide with chloroalkyl isothiocyanates
Authors: Chern Ji‐Wang , Wu Ying‐Hwa , Liu Kang‐Chien 
Published: March 2009

AbstractA reaction of 2‐aminobenzenesulfonamide (1) with 2‐chloroethyl or 3‐chloropropyl isothiocyanate in isopropanol afforded 2‐(2′‐chloroethylthioureido)‐ and 2‐(3′‐chloropropylthioureido)benzenesulfonamides (2a,b) in 67% and 55% yield respectively. Treatment of 2a,b with triethylamine in methanol at room temperature furnished 3‐(2′‐aminoethylthio)‐ and 3‐(3′‐aminopropylthio)‐2H‐1,2,4‐benzothiadiazine 1,1‐dioxides (9a,b) in quantitative yield. Heating 2b to reflux in methanol under neutral conditions gave 9b but in the form of the hydrochloride 8b which could be converted into the free base 9b by treating with ammonia water. When compounds 2a,b were treated with triethylamine in methanol at elevated temperature, 3‐(2′‐mercaptoethylamino)‐ and 3‐(3′‐mercaptopropylamino)‐2H‐1,2,4‐benzothiadiazine 1,1‐dioxides (10a,b) were obtained in good yield. Alternatively, 10a,b could also be prepared from 9a,b in 95% and 77% yield respectively.
Non‐steroidal antiinflammatory agents. VI. Synthesis of 10‐oxo‐5H‐pyrrolo[1,2‐b]isoquinoline‐3‐acetic Acid, a conformationally restricted analogue of tolmetin
Authors: Corelli Federico , Garofalo Antonio , Massa Silvio , Silvestri Romano , Prosini Pierpaolo , Artico Marino 
Published: March 2009

AbstractThe synthesis of 10‐oxo‐5H‐pyrrolo[1,2‐b]isoquinoline‐3‐acetic acid 4, a tricyclic analogue of tolmetin which might show significant analgesic‐antiinflammatory activity, has been accomplished in four steps. Alkylation of ethyl 2‐pyrrolylglyoxylate (15) with 2‐cyanobenzyl bromide afforded derivative 16, which was transformed by the Huang‐Minion reaction into the dicarboxylic acid 6. Cyclization of this key intermediate to 17, followed by alkaline hydrolysis, afforded 10‐oxo‐5H‐pyrrolo[1,2–6]isoquinoline‐3‐acetic acid (4). Various attempted syntheses of 6 are also discussed.
Some reactions of thieno‐fused quinoline N‐oxides
Authors: Gronowitz Salo , Timari Géza 
Published: March 2009

AbstractA convenient method for the conversion of the three thieno‐fused quinoline N‐oxides to the corresponding 4‐oxo‐4,5‐dihydrothienoquinolines is described. They have been alkylated with dimethylaminoethyl and dimethylaminopropyl chlorides. The reaction of the three thieno‐fused quinolines with dimethyl acetylenedicarboxylate has been studied, as well as their reactions with butyllithium and LDA.
Synthesis and antibacterial activity of 2,3‐dehydroofloxacin
Authors: Augeri David J. , Fray Andrew H. , Kleinman Edward F. 
Published: March 2009

AbstractThe 2,3‐dehydro analog 2 of the potent quinolone antibacterial agent ofloxacin (1) was synthesized by an efficient six step route beginning with ethyl 2,3,4,5‐tetrafluorobenzoylacetate. Formation of the oxazine ring of 2 was accomplished by ozonolysis of 1‐(1‐buten‐3‐yl)quinolone 5 to the corresponding aldehyde, which cyclized upon treatment with base via intramolecular displacement of the C‐8 fluorine to afford tricyclic ester 6. The antibacterial activities of 2,3‐dehydroofloxacin (2) and ofloxacin (1) are compared.
Synthesis of 3‐amino‐5H‐1,2,3‐triazino[5,4‐b]indol‐4‐one. New compounds with blood platelet antiaggregation activity
Authors: Monge A. , Aldana I. , Arrarás J. A. , Fernández‐Alvarez E. 
Published: March 2009

AbstractStarting with 3‐aminoindole‐2‐carbohydrazide 1 a series of arylidene hydrazones 2 was obtained with good yields (79–85%). Upon treating 2 with nitrous acid a series of 3‐arylidineamino‐5H‐1,2,3‐triazino[5,4‐b]indol‐4‐ones 3 was obtained (80–86%). The reaction of 4‐methoxybenzylidene derivative 3e with hydrazine hydrate, in ethanol, gave 3‐amino‐5H‐1,2,3‐triazino[5,4‐b]indol‐4‐one 4 (64%). However, by treating 3e in boiling hydrate, 3‐aminoindole‐2‐carbaldehyde azine 5 was obtained (44%). By boiling 1 in N,N‐dimethylformamide, 3‐amino‐5H‐pyrimido[5,4‐b]indol‐4‐one, 6 was obtained (52%).
Isolation of 1,2,3,4‐tetrahydrobenzo[f]quinolin‐2‐ones on the reaction of 2‐arylidenenaphthylamines with 4‐hydroxycoumarin. IV
Authors: Martínez Roberto , Cortés Eduardo , Toscano Rubén A. , Alfaro L. Josué , Avila J. Gustavo 
Published: March 2009

AbstractThe reaction of 2‐arylidenenaphtylamines with 4‐hydroxycoumarin results in Hoffman‐Martius type rearrangement yielding 2H‐benzo[f][1]benzopyrano[4,3‐b]quinolin‐2‐ones I and the compounds II. This work describes the structure elucidation of the compounds II. The structure was confirmed using ir, nmr and X‐ray spectroscopy.
Synthesis and spectroscopic characterization of 1‐[1,2,3‐triazol‐1‐yl]‐4‐aroylazetidin‐2‐ones
Authors: Bojilova Anka , Rodios Nestor A. 
Published: March 2009

Abstract1‐(N‐Phenacylidene)amino‐1,2,3‐triazoles 3 react with propionylchloride and phenoxyacetylchloride in the presence of triethylamine to give trans‐ (5) and cis‐ (6) 1‐(1,2,3‐triazol‐1‐yl)‐4‐aroylaztidin‐2‐ones in a 1:1 ratio, on the contrary to the 1‐(N‐arylidene)amino‐1,2,3‐triazoles, which do not give any reaction product with the same acid chlorides. The spectroscopic characteristics of these new N‐triazolyl‐β‐lactams are also discussed.
1,3‐Dipolar cycloadditions of nitrile oxides with 4‐carbethoxymethyleno‐4,5,6,7‐tetrahydro‐6,6‐dimethylbenzo[c][1,2,5]oxadiazole
Authors: Koumbis Alexandros E. , Stephanidou‐Stephanatou Julia , Alexandrou Nicholas E. 
Published: March 2009

AbstractThe (E)‐ and (Z)‐α,β‐unsaturated esters, 3 and 4 are prepared by applying a Wittig reaction on the ketone 1. Stable nitrile oxides are added to the stable (E)‐isomer 3 resulting to the formation of the spiro‐derivatives 7, whereas with the unstable nitrile oxides a second stereoisomer 8 is also formed. Mesitonitrile oxide reacts also with the ketone 1 to give the spiro‐cycloadduct 10. The assignment of regio‐isomers 7 was deduced from their spectral data as well as from some molecular orbital considerations.
Quinolone antibacterials. 2. 6‐Substituted‐7‐(2‐thiazolyl and thiazolidinyl)quinolones
Authors: Zhang M. Q. , Haemers A. , Vanden Berghe D. , Pattyn S. R. , Bollaert W. , Levshin I. 
Published: March 2009

AbstractA series of 6‐substituted‐1‐ethyl‐1,4‐dihydro‐4‐oxo‐7‐(2‐thiazolyl‐ and thiazolidinyl)quinoline‐3‐carboxylic acids were synthesized. Substitution at the 6‐position was H, F or Cl. The Hantzsch method was used for the preparation of the thiazolylquinolones. The thiazolidinylquinolones were synthesized by quaternization of the corresponding thiazolyl analogues, followed by reduction of the obtained thiazolium salts with sodium borohydride in aqueous solution. Antibacterial activity was tested in vitro. The compounds were inactive against Gram‐negative bacteria but some of them showed good activity against Gram‐positive bacteria and mycobacteria. This activity pattern is rarely found among the quinolone antibacterials.