bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of 1,2:5,6‐Di‐O‐isopropylidene‐3‐O‐[3‐(5‐fluorouracil‐1‐yl)‐propionoyi]‐α‐D‐glucofuranose and its antitumor activity
Authors: Ouchi Tatsuro , Jokei Satoshi , Fujie Hirotoshi , Chikashita Hidenori , Inoi Takeshi 
Published: April 2009

AbstractIn order to provide a less toxic 5‐fluorouracil derivative, 1,2:5,6‐di‐O‐isopropylidene‐3‐O‐[3‐(5‐fluorouracill‐yl)‐propionoyl]‐α‐D‐glucofuranose, which was the derivative of 5‐fluorouracil combining indirectly to 3‐position of diacetoneglucose, was synthesized, and its antitumor activity was tested.
New heterocyclic syntheses from hydrazidoyl halides. Convenient syntheses of fused pyrimidines, pyridazines, and quinazolines
Authors: Abdehamid Abdou O. , PÁrkÁnyi Cyril , Shawali Ahmad S. , Abdalla Magda A. 
Published: April 2009

AbstractAminocyanopyrazole derivatives and pyrazolo[2,3‐a]quinazolones were obtained in good yields from hydrazidoyl halides and malononitrile. Pyrazolo[3,4‐d]pyridazine and pyridazo[4′,5′: 1,2]pyrazolo[1,5‐a]quinazoline derivatives were synthesized in quantitative yields by reaction of hydrazine hydrate with 2 and 16, respectively. A novel ring system, a 3‐substituted tetrahydro derivative of 7‐oxo‐6H,8H‐pyridazo[3′,4′,5′‐c'd']‐pyrazolo[3,4‐d]pyrimidine was prepared by reaction of 6 with dimethyl carbonate. Pyrazolo[3,4‐d]pyrimidine‐4,6‐dithiones were obtained in good yields by reaction of 2 with carbon disulfide. The structures of the products were assigned and confirmed on the basis of their elemental analyses, spectral data, and alternate synthesis wherever possible. The structures of the parent fused heterocyclic systems discussed in this work are summarized in Scheme 1.
Phase transfer catalyzed synthesis of indazoles from o‐alkylbenzenediazonium tetrafluoroborates
Authors: Bartsch Richard A. , Yang Il‐Woo 
Published: April 2009

AbstractReactions of o‐methyl‐ and o‐ethylbenzenediazonium tetrafluoroborates with two equivalents of potassium acetate and five mole percent of 18‐crown‐6 in ethanol‐free chloroform produce indazoles in good to excellent yields. Indazoles bearing either electron‐withdrawing or electron‐donating substituents may be prepared.
Benzo[b]thiophene. Derivatives. XXVIII. 5‐bromo‐3‐benzo[b]thienylalanine and derivatives
Authors: Campaigne E. , Kim Chung S. 
Published: April 2009

AbstractA potential inhibitor of gelation of sickle hemoglobin, 5‐bromo‐3‐benzo[b]thienylalanine, has been synthesized along with several derivatives. Several hydrolytic pathways from the intermediate ethyl 5‐bromo‐3‐benzo[b]thienylformamidomalonate have been examined, and that involving alcoholysis to ethyl N‐formyl‐5‐bromo‐3‐benzo[b]thienylalanine shown to be superior.
Polarographic reduction and tautomeric structure of 2‐amino‐5‐arylazothiazoles
Authors: Elanadouli Bahgat E. , Abdelhamid Abdou O. , Shawali Ahmad S. 
Published: April 2009

AbstractThe polarographic behaviour of a series of 2‐amino‐4‐phenyl‐5‐arylazothiazoles has been investigated at a dropping mercury electrode. Each of the compounds studied exhibits one wave which was shown to correspond to the reductive cleavage of the azo linkage by a 4e irreversible step. On the basis of the polarographic data, it was concluded that the compounds exist only in one tautomeric form, namely the aminoazo structure 1. The results of E1/2 — σX correlations and HMO calculations of bonding energies of the various possible tautomeric forms 1–3 indicate that the aminoazo form 1 is the most stable structure of the compounds examined.
Heterocycles of biological importance. Part 1. Novel synthesis and biological activity study of 5‐Alkyl and 5‐Aryl‐7‐aminopyrazolo[1,5‐a]‐pyrimidines from allenic or acetylenic nitriles and 3‐aminopyrazole
Authors: Fomum Z. Tanee , Asobo P. Forche , Ifeadike P. Ngozi 
Published: April 2009

AbstractAllenic nitriles react with 3‐aminopyrazole in ethanol or dimethylformamide to give 5‐alkyl‐7‐aminopyrazolo[1,5‐a]pyrimidines5of pharmaceutical interest in good yields. 3‐Phenylpropynenitrile reacts with 3‐aminopyrazole in a similar manner to give the aryl compound8.
Chemistry of thienopyridines. XXXII. Direct introduction of C‐substituents gamma to the heteronitrogen atom in the thieno[2,3‐b]pyridine system
Authors: Klemm L. H. , Muchiri Daniel R. , Louris John N. 
Published: April 2009

AbstractTreatment of the N‐oxide 1a of thieno[2,3‐b]pyridine (1) with either (a) acetic anhydride and ethyl cyanoacetate or (b) benzoyl chloride and an enamine of cyclohexanone (Hamana reactions) serves to introduce a C‐substituent at the 4‐position of 1. In case (a) one obtains a yellow, isolable vinylogous N‐ylide 5 (23% yield), which undergoes facile transformation into ethyl 2‐(4‐thieno[2,3‐b]pyridyl)cyanoacetate (1e) (88–93 %). Acetic anhydride reconverts 1e to 5 (95%). Case (b) produces 2‐(4‐thieno[2,3‐b]pyridyl)cyclohexanone (39%), hydrolyzable to 6‐(4‐thieno[2,3‐b]pyridyl)hexanoic acid (45%). The hydrochloride of 1a is also reported. Structural formulations are based on spectral studies (including 13C nmr data for 1 and 1e) and chemical transformations. Major contrasts (plus some similarities) between the systems 1 and quinoline in the Hamana reactions are discussed.
Shift reagent 1H NMR study of methoxycoumarins
Authors: Joseph‐Nathan P. , DomÍnguez M. , Ortega D. A. 
Published: April 2009

AbstractThe complete assignment of the proton chemical shifts of coumarin (1), all monomethoxy derivatives and the six possible dimethoxyl substituted compounds at the aromatic ring was achieved at 60 MHz in a quantitative study utilizing Pr(fod)3 as the shift reagent. It was found that in addition to the complexation at the lactone carbonyl a second interaction of the lanthanide shift reagent occurs when two methoxyl groups are found in an ortho distribution. The results are discussed in comparison to data published for flavones in the presence of Pr(fod)3 shift reagent.
Bromination of methyl substituted 1,2,5‐thiadiazoles with N‐bromosuccinimide
Authors: Mataka Shuntaro , Kurisu Masayoshi , Takahashi Kazufumi , Tashiro And Masashi 
Published: April 2009

AbstractBromomethyl‐1,2,5‐thiadiazoles 2a‐c were prepared by bromination of methyl‐1,2,5‐thiadiazoles 1a‐c by NBS in refluxing carbon tetrachloride. When bromination of 1a and 1b was carried out under irradiation of tungusten lamp, mixtures of cis‐5a and b and trans‐1,2‐dibromo‐1,2‐bis(1,2,5‐thiadiazol‐3‐yl)ethylene (6a and b) were obtained.
13C NMR spectra of 1‐(α‐aroyloxyarylideneamino)‐1,2,3‐triazoles. Identification of 4,5‐unsymmetrically substituted derivatives
Authors: Rodios Nestor A. 
Published: April 2009

AbstractThe 13C nmr spectra of the title compounds are reported. Chemical shifts of C‐4 and C‐5 carbons of the triazole ring are used for structural assignment of the 4,5‐unsymmetrically substituted 1‐(α‐aroyloxyarylideneamino)‐v‐triazoles (triazolylisoimides). A complete assignment of the shifts of the α‐aroyloxyarylideneamino group is given. Some JC‐H values are also reported.
A Convenient Synthesis of 2‐N‐Methoxycarbonylaminooxazolo[5,4‐d]pyrimidines
Authors: Chern Ji‐Wang , Wise Dean S. , Townsend Leroy B. 
Published: April 2009

AbstractA facile synthesis of methyl oxazolo[5,4‐d]pyrimidine‐2‐carbamic acids by the cyclodesulfurization of a methoxycarbonyl thiourea with dicyclohexylcarbodiimide is described.
The synthesis of pyrazolo[3,4‐d]pyridazines. Photochemical cyclization to pyrazolo[3,4‐d]pyridazin‐4(5H)‐ones with subsequent functionalization
Authors: Kaji Kenji , Nagashima Hiromu , Ohta Yusho , Tabashi Keizo , Oda Hirohisa 
Published: April 2009

AbstractThe synthesis of 1,3‐disubstituted and 1,3,5‐trisubstituted 1H‐pyrazolo[3,4‐d]pyridazin‐4(5H)‐ones is conveniently performed by photochemical cyclization. Functionalization of the former compounds leading to the formation of 1,4‐disubstituted and 1,3,4‐trisubstituted 1H‐pyrazolo[3,4‐d]pyridazines is smoothly effected through pertinent nucleophilic substitutions.
Synthesis of 7‐substituted 1H‐indolo[3,2‐d][1,2]benzoxazepines
Authors: Klioze Sol S. , Ehrgott Frederick J. , Glamkowski Edward J. 
Published: April 2009

AbstractThe synthesis of the novel 7‐substituted 1H‐indolo[3,2‐d][1,2]benzoxazepine ring system is described. Fischer indolization of 2‐fluoroacetophenone phenylhydrazone provided the starting material 2‐(2‐fluorophenyl)‐1H‐indole. An acyl group was then introduced at the 3‐position of the indole nucleus and the resulting ketone was converted to the ketoxime. Upon treatment with sodium hydride to form the oxanion of the ketoxime, an intramolecular cyclization took place via displacement of fluoride from the adjacent 2‐fluorophenylsubstituent. This ring closure completed the construction of the 1H‐indolo[3,2‐d][1,2]benzoxazepine ring system.
Synthesis of 7‐azadispiro[5.1.5.2]pentadecane and 6‐azadispiro[4.1.5.2]tetradecane
Authors: Wagner E. R. , Matthews D. P. 
Published: April 2009

AbstractTwo new, hindered secondary amines, 7‐azadispiro[5.1.5.2]pentadecane hydrochloride (1a) and 6‐azadispiro[4.1.5.2]tetradecane hydrochloride (1b), have been prepared in four steps from 1‐ethynylcyclohexylamine (2). The final thermal cyclization of 1‐(2‐(1‐aminocyclohexyl)ethyl)cyclohexyl chloride (5a) produces 1‐(2‐(1‐aminocyclohexyl)ethyl)cyclohexene hydrochloride (6a) and an unsaturated hydrocarbon 7 in addition to 1a.
Nitrogen bridgehead compounds. Part 45 [1]. Synthesis of 6‐arylhydrazono‐6,7,8,9‐tetrahydro‐11H‐pyrido‐[2,1‐b]quinazolin‐11‐ones
Authors: Kökösi József , Szász György , Hermecz István , Podányi Benjámin , Mészáros And Zoltan 
Published: April 2009

AbstractA series of 6‐arylhydrazono‐6,7,8,9‐tetrahydro‐11H‐pyrido[2,1‐b]quinazolin‐11‐ones 3–37, conveneint starting materials for indolopyridoquinazolines, were prepared by diazonium coupling between aryldiazonium chlorides and 6,7,8,9‐tetrahydro‐ 2, 6‐formyl‐5,7,8,9‐tetrahydro‐ 39, 6‐(dimethylamino)methylene‐6,7,8,9‐ 38 or 6‐carboxyl‐5,7,8,9‐tetrahydro‐11H‐pyrido[2,1‐b]quinazolin‐11‐ones 43. The arylhydrazono derivatives were also prepared from 6‐bromo‐ 45 or 6,6‐dibromo‐6,7,8,9‐tetrahydro‐11H‐pyrido[2,1‐b]quinazolines 46 with arylhydrazines. The structures of the 6‐arylhydrazonopyridoquinazolines were characterized by uv and 1H nmr spectroscopy. The 6‐arylhydrazono derivatives show a solvent‐dependent E‐Z isomerism.
5‐Cyano‐6‐aryluracil and 2‐thiouracil derivatives as potential chemotherapeutic agents. IV
Authors: Ram Vishnu J. , Berghe D. A. Vanden , Vlietinck A. J. 
Published: April 2009

AbstractA series of 5‐cyano‐6‐aryluracils and 2‐thiouracils1a‐hhas been prepared and alkylated to 1,3‐dialkyluracils2a‐dand 2‐alkylthiouracils,3, 4and6, by electrophilic substitution with alkyl halides. Reaction of1bwith dibromoethane and 1,3‐dibromopropane gave the corresponding bicyclic products, 7‐aryl‐6‐cyano‐2,3‐dihydrothiazolo[3,2‐a]pyrimidin‐5‐ones5a,band 8‐aryl‐7‐cyano‐3,4‐dihydro‐2H‐pyrimido[2,3‐b][1,3]thiazin‐6‐ones5c‐g. Nucleophilic substitution on6with hydrazine led to7which on refluxing with formic acid gave 5‐aryl‐6‐cyano‐8‐methyl‐s‐triazolo[3,4‐b]pyrimidin‐7‐ones (9), while with acetic and propionic acids only 2‐acylhydrazino‐3‐methyl‐4‐oxo‐5‐cyano‐6‐arylpyrimidines8a,bwere isolated. The hydrazine7undergoes cyclization with acetylacetone and methyl dimethylmercaptoacrylate providing 2‐(pyrazol‐1‐yl)‐3‐methyl‐4‐oxo‐5‐cyano‐6‐substituted pyrimidines10, and11. Some of the compounds were screened for antibacterial‐, antifungal‐ and antiviral activities and a few of them showed significant chemotherapeutical activities.
Synthesis of 7‐(1‐pyrrolidinyl)‐1,2,4‐triazolo[4,3‐b]pyridazines
Authors: Peet Norton P. 
Published: April 2009

AbstractThe reactions of secondary amines (pyrrolidine, piperidine and morpholine) with 3,4,5‐trichloropyridazine (4) was investigated. With 4 and excess amine, disubstitution occurred in good yield and selectively at positions 3 and 5. Treatment of 4 with 2 equivalents of the amine in ethanol afforded high yields of products resulting from monosubstitution at position 5. 3,4‐Dichloro‐5‐(1‐pyrrolidinyl)pyridazine (6a), resulting from 4 and 2 equivalents of pyrrolidine, was converted cleanly to 4‐chloro‐3‐hydrazino‐5‐(1‐pyrrolidinyl)pyridazine (8) with hydrazine hydrate. Pyridazine 8 was cyclized with formic acid to give a 1:1 complex (9) of formic acid and 8‐chloro‐7‐(1‐pyrrolidinyl)‐1,2,4‐triazolo[4,3‐b]pyridazine (13). Triazolopyridazine 13 also formed a monohydrate (12) and a monohydrochloride salt (14). Catalytic hydrogenation of 9 gave 7‐(1‐pyrrolidinyl)‐1,2,4‐triazolo[4,3‐b]pyridazine (3), which was a target compound of this investigation.
Reactions of derivatives of anthranilic acid with 3‐chloropropyl isocyanate
Authors: Papadopoulos E. P. 
Published: April 2009

AbstractThe urea 1 obtained from anthranilonitrile and 3‐chloropropyl isocyanate is converted into 3‐(3‐chloropropyl)‐2,4(1H,3H)quinazolinedione (4) when heated with hydrochloric acid, whereas it undergoes a double cyclization to form 2,3,4,7‐tetrahydro‐6H‐pyrimido[1,2‐c]quinazolin‐6‐one (3) upon heating, or treatment with ammonia. On the other hand, the urea 5 formed from methyl anthranilate and 3‐chloropropyl isocyanate cyclizes in three different ways, when treated with ammonia, potassium bicarbonate, or concentrated sulfuric acid, to yield compound 4, 3,4‐dihydro‐2H,6H‐[1,3]oxazino[2,3‐b]quinazolin‐6‐one (9), or 2‐[(3‐chloropropyl)amino]‐4H‐3,1‐benzoxazin‐4‐one (6), respectively. Acid‐catalyzed reactions of compound 9 with nucleophilic reagents proceed with opening of the oxazine ring and readily yield various 3‐substituted 2,4(1H,3H)‐quinazolinediones.
Radical cation formation and crystal structure determination of 4′‐dimethylamino‐10‐phenylpyrido[3,2‐b]benzothiazine
Authors: Jovanovic Misa V. , Biehl Edward R. , De Meester Patrice , Chu Shirley S. C. 
Published: April 2009

AbstractThe crystal structure of title compound, 4, shows that the 10‐aryl group is parallel to the plane bisecting the pyridobenzothiazine ring. This structure is in contrast to that normally found for phenothiazines substituted with electron‐withdrawing substituents on the 10‐phenyl ring. In those compounds, the 10‐aryl group is perpendicular to the plane bisecting the phenothiazine ring. The esr spectrum of the cation radical of 4 shows that the radical is located on the hetero ring system which is opposite to that of the cation radical of 4′‐dimethylamino‐10‐phenylphenothiazine in which the radical is located on the 10‐aryl ring.
Pyrrolothienopyrazines: étude chimique de la pyrrolo[1,2‐a]‐thiéno[3,2‐e]pyrazine
Authors: Rioult Jean‐Philippe , De Sévricourt Michel Cugnon , Rault Sylvain , Robba Max 
Published: April 2009

AbstractLa réactivité de la pyrrolo[1,2‐a]thiéno[3,2‐e]pyrazine 1 est étudiée vis‐à‐vis des réactions de quaternarisation, bromation, nitration, Friedel Crafts, Vilsmeier Haack, sulfonation et de Reissert. La structure des produits obtenus est déduite de l'analyse de leur spectre de rmn ou de masse. Les mélanges ont été étudiés par chromatographie en phase gazeuse couplée à la spectrométrie de masse (gc/ms).
Some derivatives of morpholinophosphorodichloridate and dichloridothioate
Authors: Cremlyn Richard J. , Patel Kantilal , Wu Luke 
Published: April 2009

AbstractMorpholinophosphorodichloridate and dichloridothioate reacted with amines (2 molar equivalents) to give the amidic chlorides which were treated with nucleophilic reagents to give sixty‐four derivatives. However the dichloridothioate with primary amines (1 molar equivalent) only gave diamidic thioates, the reasons for the failure to obtain the expected amidochloridothioates are briefly discussed.
Novel synthesis of isoxazolo[5,4‐b]quinolines
Authors: Neelima  , Bhat Balkrishen , Bhaduri Amiya Prasad 
Published: April 2009

AbstractIsoxazolo[5,4‐b]quinolines have been prepared by reacting 3‐acyl or aroyl‐2‐chloro‐6‐alkoxy or 6,7‐dialkoxyquinolines with hydroxylamine. The method is of general applicability for obtaining this class of compounds and involves the use of easily available starting materials.
Heterocycles. Part V. Reaction of α,β‐unsaturated carbonyl compounds with arylacetamides. A synthesis of 2‐pyridone derivatives
Authors: El‐Rayyes N. R. , Al‐Hajjar F. H. 
Published: April 2009

AbstractThe reaction of 1,3‐diaryl‐2‐propene‐1‐ones I with arylacetamides II, in the presence of sodium ethoxide under reflux, for two hours, gave the corresponding 3,4,6‐triaryl‐3,4‐dihydro‐2(1H)‐pyridones IV. However, when the reaction of these ketones was carried out in the presence of sodium hydride, they gave the corresponding 3,4,6‐triaryl‐2(1H)‐pyridones VI or a mixture of IV and VI. When 1,3‐diaryl‐2‐propyne‐1‐ones V were reacted with arylacetamides, in the presence of sodium hydride, they yielded the corresponding 2‐pyridones VI. Treatment of compounds IV with selenium produced the corresponding 2‐pyridones VI. Acetylation of the latter compounds gave the corresponding 2‐acetyl derivatives VIII. The structure of all products was confirmed by chemical and spectroscopic evidence, and the mechanism of the reactions was discussed.
Synthèse et étude structurale du N‐méthyl‐aza‐10‐bicyclo[4,3,1]decane‐8‐spiro‐5′‐hydantoïne
Authors: Trigo G. Gonzalez , Muñoz E. Martínez , Llama‐Hurtado E. 
Published: April 2009

AbstractOn décrit pour la première fois la synthèse de la spirohydantoïne derivée du N‐méthyl‐homogranatane [N‐méthyl‐aza‐10‐bicyclo[4,3,1]decane] avec centre spiranique en C‐8. Nous avons attribué la configuration α à ce centre. La conformation et les associations que cette molécule présente à l'état solide ont été étudiées en les comparant avec celles des homologues inférieurs. Quelques bases de Mannich ont également été préparées.
Synthèse de β‐imidazolylcétones
Authors: Montignoul Claude , Richard Marie‐Josée , Vigne Christian , Giral Louis 
Published: April 2009

AbstractNous décrivons la synthèse de β‐imidazolylcétones 1 et 2. Les composés 1 sont obtenus par action de l'imidazole sur des β‐N,N‐diméthylaminocétones obtenues au préalable par réaction de Mannich. Les composés 2 sont préparés soit par alkylation directe de l'imidazole par une β‐halogénocétone ou une cétone α‐éthylénique, soit par action du β‐cétol sur le thionyldiimidazole.
Utilisation des plans factoriels fractionnaires pour l'étude de la réaction de bucherer‐bergs: Synthèse de la cyclohexane spirohydantoîne
Authors: Pedregal Carmen , Trigo Gregorio G. , Espada Modesta , Mathieu Didier , Tan Luu Roger Phan , Barceló Carlos , Lamarca Joaquin , Elguero José 
Published: April 2009

AbstractL'utilisation d'une matrice factorielle fractionnaire de seulement seize expériences permet d'étudier l'effet de sept facteurs (volume du récipient, concentrations en cyanure et en carbonate d'ammonium, volumes d'eau et d'éthanol, température et temps de réaction) sur le rendement en cyclohexane spirohydantoïne. La stratégie expérimentale et les résultats sont comparés avec ceux d'une publication récente utilisant la méthode d'optimisation du Simplex, montrant une connaissance plus précise de la réaction après une matrice factorielle.
Synthesis of 3‐amino‐2,4(1H,3H)‐quinazolinediones for testing as anticonvulsants
Authors: Kornet M. J. , Varia T. , Beaven W. 
Published: April 2009

AbstractA number of 3‐amino‐2,4(1H,3H)‐quinazolinediones were synthesized from o‐aminobenzoylhydrazines and ethyl chloroformate in pyridine or from 2‐methoxycarbonylphenyl isocyanate and 1,1‐disubstituted hydrazines. Four of the ten compounds screened exhibited anticonvulsant activity in mice.
Synthesis of 1,2,3,4‐tetrahydro‐5H‐[1]benzopyrano[3,4‐c]pyridin‐5‐ones. I. 3‐unsubstituted compounds
Authors: Connor David T. , Unangst Paul C. , Schwender Charles F. , Sorenson Roderick J. , Carethers Mary E. , Puchalski Chester , Brown Richard E. 
Published: April 2009

AbstractSynthesis of 1,2,3,4‐tetrahydro‐5H‐[1]benzopyrano[3,4‐c]pyridin‐5‐ones via a Pechmann condensation of 3‐carbethoxy‐1‐methyl‐4‐piperidone with various phenols is described. The limitations of this method are discussed. Synthesis of the parent ring system 3a via reduction of 1,2,3,4‐tetrahydro‐3‐(phenylmethyl)‐8‐[(1‐phenyl‐1H‐tetrazol‐5‐yl)oxy]‐5H‐[1]benzopyrano[3,4‐c]pyridin‐5‐one (5) is also described.
Synthesis of fluorescent and coloured pyrylium and pyridinium salts
Authors: Katritzky Alan R. , Schwarz Otto A. , Abdel Rahman Abdu E. , Leahy David E. 
Published: April 2009

AbstractThe synthesis is described of fluorescent and coloured pyrylium and pyridinium salts, including water‐soluble derivatives, designed to serve as marker reagents for primary amines.
Ring transformation of 5‐aroyl‐3(2H)‐isothiazolones to 1,2,5‐oxathiazole and 1,2,3‐thiadiazole derivatives
Authors: Tsolomitis A. , Sandris C. 
Published: April 2009

AbstractReaction of 2‐substituted‐5‐aroyl‐3(2H)‐isothiazolones 2 with hydroxylamine and phenylhydrazine was found to give (N‐substituted‐carboxamido)methylene derivatives of 1,2,5‐oxathiazole and 1,2,3‐thiadiazole, 5 and 7, respectively. The formation of these heterocycles was ascribed to a mononuclear heterocyclic rear‐rangement of the initially formed ketone derivatives, oximes and hydrazones, through a nucleophilic attack of the = N‐OH and = N‐NH‐ groups on the SN bond of the isothiazolone ring. In a similar manner, reaction of isothiazolones 2 with hydrazine was found to give 4‐aryl‐5‐(N‐substituted‐carboxamido)methyl‐1,2,3‐thiadiazoles 17.
Synthesis of 3‐amino‐3,4‐dihydro‐2(1H)‐quinazolinones as potential anticonvulsants
Authors: Kornet M. J. , Varia T. , Beaven W. 
Published: April 2009

AbstractThirteen 3‐amino‐3,4‐dihydro‐2(1H)‐quinazolinones have been synthesized from ethyl chloroformate and o‐aminobenzylhydrazines. The latter compounds were obtained from the metal hydride reduction of either o‐aminobenzhydrazides or o‐acylaniline hydrazones. All compounds were evaluated in mice in the maximal electroshock (MES) seizure and pentylenetetrazole (sc Met) seizure threshold tests for anticonvulsant activity and in the rotorod test to determine neurotoxicity. Five of the compounds showed activity in one or both tests at a dose of 300 mg/kg or lower. The most active compound is 3‐dimethylamino‐3,4‐dihydro‐2(1H)‐quinazolinone.
Non‐steroidal antiinflammatory agents. 2. Synthesis of 4‐hydroxy‐1‐methyl‐2‐oxo‐dihydroquinolin‐3‐yl acetic acid and related tetrazolyl derivatives
Authors: Faber Kurt , Kappe Thomas 
Published: April 2009

AbstractThe synthesis of some potential antiinflammatory compounds, such as the tetrazole derivatives 7 and 9, as well as the heteroaryl acetic acid 12 and its lactone 13, has been accomplished starting from the readily available pyronoquinolone 2.
Activated nitriles in heterocyclic synthesis. Part III. Synthesis of N‐amino‐2‐pyridone, pyranopyrazole and thiazolopyridine derivatives
Authors: Elmoghayar Mohamed Rifaat Hamza , El‐Agamey Abdel‐Ghani Ali , Nasr Mohamed Yousri Abdel‐Samad , Sallam Mohamed Mohamed Mohamed 
Published: April 2009

AbstractThe reaction of 2‐cyanoethanoic acid hydrazide and arylidenemalononitrile was studied as a new route for the synthesis of N‐amino‐2‐pyridones. Pyrano[2,3‐c]pyrazole and thiazolo[2,3‐a]pyridine could be prepared from the reaction of arylideneazolones with the same reagent.
A novel serotonin antagonist 2,2′‐bis[3‐(2‐N,N‐dimethylaminoethyl)indolyl]sulfide (BDIS)
Authors: Chu C. K. , Wander J. D. , Tackett R. L. , Iturrian W. B. , Schmitz J. P. , Garner G. E. , Chae K. 
Published: April 2009

AbstractA novel serotonin antagonist, 2,2′‐bis[3‐(2‐N,N‐dimethylaminoethyl)indolyl]sulfide (BDIS) was synthesized in one step from the reaction ofN,N‐dimethyltryptamine with thionyl chloride.
An unexpected product from the reaction of imidazole with ethyl 3‐ethoxy‐2‐nitropropenoate
Authors: Hartman George D. , Hartman Richard D. 
Published: April 2009

AbstractTreatment of ethyl 3‐ethoxy‐2‐nitropropenoate with imidazole afforded ethyl 1‐imidazoyl(hydroximino)‐acetate rather than the expected addition‐elimination product.