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通过3-苄基-4-芳酰基-1,2,4-三唑-5-巯基负离子在2-甲磺酰基-5-苯基-1,3,4-噁二唑环2-位上的亲核取代反应,制得13个新的(3-苄基-4-芳酰基-1,2,4-三唑-5-基)(5-苯基-1,3,4-噁二唑-2-基)硫醚衍生物.经元素分析、IR、~1H NMR和MS裂解碎片分析确认结构.初步观察了它们在0.01%浓度时对大肠杆菌繁殖的抑制作用. 相似文献
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Lyubov' N. Sobenina Vladislav N. Drichkov Al'bina I. Mikhaleva Olga V. Petrova Igor A. Ushakov Boris A. Trofimov 《Tetrahedron》2005,61(20):4841-4849
5-Amino-3-(pyrrol-2-yl)isoxazoles were selectively prepared by the reaction of 2-(2,2-dicyano-1-ethylthioethenyl)pyrroles with hydroxylamine in methanol. Under analogous conditions, 2-(2-carbamoyl-2-cyano-1-ethylthioethenyl) pyrroles with hydroxylamine gave 5-aminoisoxazoles and their structural isomers, 3-aminoisoxazoles (3-5% yield). The latter were selectively prepared by reacting 2-(2-carbamoyl-2-cyano-1-ethylthioethenyl)pyrroles with hydroxylamine in the presence of aqueous NaOH and from the products of intramolecular cyclization of 2-(2-carbamoyl-2-cyano-1-ethylthioethenyl)pyrroles, 1-ethylthio-3-iminopyrrolizines and hydroxylamine. 相似文献
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Based on a computer-assisted analysis of the three-dimensional structure of the binary complex of E.coli dihydrofolate reductase (DHFR) with methotrexate, 5-(N-arylnortropan-3-yl)- and 5-(N-arylpiperidin-4-yl)-2,4-diaminopyrimidines 2 and 4 were designed as inhibitors of DHFR. Syntheses of the designed compounds have been carried out. The most potent compound 2a inhibited E. coli DHFR with Ki = 0.49.10?9M. The activities within the series of compounds synthesized could be rationalized by molecular-modelling experiments which served as the basis of this work. Several compounds within the presented series exhibit antimalarial activities in vitro and in vivo. 相似文献
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A facile transformation of 2- and 3-methylcarbazoles into 3-(carbazol-2-yl)-and 3-(carbazol-3-yl)-dl-alanines compounds is described. 相似文献
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V. I. Potkin N. A. Bumagin A. V. Kletskov S. K. Petkevich P. V. Kurman 《Russian Journal of Organic Chemistry》2016,52(11):1661-1669
From (4,5-dichloroisothiazol-3-yl)phenylmethanol by Ritter reaction a substituted acetamide was synthesized that at hydrolysis with HCl afforded (4,5-dichloroisothiazol-3-yl)phenylmethylamine hydrochloride. By reaction of (5-arylisoxazol-3-yl)- and 4,5-dichloroisothiazol-3-yl)arylmethanol with thionyl chloride the corresponding (1,2-azol-3-yl)arylchloromethanes were obtained. At treatment with O- and N-nucleophiles chlorine atom in chloromethylеne fragment of obtained compounds was substituted by residues of benzylamine, morpholine, vanillin, and ethoxy group. 相似文献
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A general method was proposed for the synthesis of 3-(5-aryl-1,3,4-oxadiazol-2-yl)chromones starting from 3-formylchromone. This aldehyde yields acylhydrazones, from which the corresponding unstable nitrile imines are generated. These intermediates undergo intramolecular 1,3-dipolar cycloaddition. 相似文献
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A general procedure was proposed for the synthesis of 3-(5-aryl-1,3,4-oxadiazol-2-yl)chromones by reaction of 3-formylchromone with aroylhydrazines, transformation of the corresponding acylhydrazones into 1,3-dipoles by the action of bromine in the presence of sodium acetate, and intramolecular ring closure. 相似文献
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4-(5-喹啉-3-基-四氮唑-2-基)丁胺的合成 总被引:1,自引:0,他引:1
三苯基膦钯催化3-溴喹啉完成氰化取代制得3-氰喹啉(1);1与叠氮化钠经[2+3]环加成合成了3-(2H-四氮唑-5-基)喹啉(2);2与N-(4-溴丁基)邻苯二甲酰亚胺反应制得2-[4-(5-喹啉-3-基-四氮唑-2-基)丁基]异吲哚-1,3-二酮(3);3经肼解合成了4-(5-喹啉-3-基-四氮唑-2-基)丁胺(4... 相似文献
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Ramiro Araya-Maturana Jorge Heredia-Moya Hernán Pessoa-Mahana Boris Weiss-López Juan Carlos Muñoz 《Acta Crystallographica. Section C, Structural Chemistry》2005,61(4):o237-o239
The title compound, C12H7NO3, consists of a chromone moiety substituted in position 3 with an acrylonitrile group in a Z configuration. The two planar groups are twisted with respect to one another. The only significant hydrogen bond in the structure is an intramolecular O—H·O bond. π–π contacts connecting aromatic groups and C—H·O intermolecular weak interactions lead to a supramolecular layer arrangement. 相似文献
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A short and efficient synthesis of 1-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(5-(2-morpholinoethoxy)-2H-chromen-8-yl) urea derivatives (1a–c), a novel type of p38 MAPK inhibitors, is described. The Claisen thermal rearrangement of arylpropargyl ethers was employd as a key step to synthesize the chromene core. The solvent effect on the ratio of the resultant two isomers of Claisen thermal rearrangement, namely 2-methylbenzofuran and 2H-chromen, was also investigated. 相似文献
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Alex F. C. Flores Juliana L. Malavolta Leandro M. Frigo Morgana Doneda Darlene C. Flores 《合成通讯》2013,43(10):1198-1204
We develop an efficient method to synthesize novel propionyl-spaced bisheterocyclic compounds. It entails cyclocondensation of 3-(5-trifluoromethyl-1H-pyrazol-3-yl)propanoyl hydrazide obtained from levulinic acid, with 1,1,1-trifluoro-4-methoxy-3-alken-2-ones proceeding regiospecifically to 1-[(5-trifluoromethyl-5-hydroxy-3-substituted-4,5-dihydro-1H-pyrazol-1-yl)-3-(5-trifluoromethyl-1H-pyrazol-3-yl)propan-1-one derivatives. 相似文献
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The 13C NMR spectra of twelve 3-aryl-4-(5-aryl-Δ2-l,2,4-oxadiazolin-3-yl)sydnones and twelve 3-aryl-4-(5-aryl-l,2,4-oxadiazol-3-yl)sydnones have been measured and assigned by means of proton-noise decoupling and DEPT-experiments. The coupling constants were determined by means of gated decoupling, and NOE effects were observed by comparison of proton-decoupled and inverse-gated decoupled spectra. Differences shown by the oxadiazoline and the oxadiazole rings and the substitution effects are discussed. 相似文献
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Condensation of 3-chloropentane-2,4-dione with thioamides gives 1-(thiazol-5-yl)ethanones and subsequent Wittig olefination, followed by nitrile oxide 1,3-dipolar cycloaddition to the resulting prop-1-en-2-yl moiety, delivers racemic 5-(thiazol-5-yl)-4,5-dihydroisoxazoles. When this thiazole and isoxazoline diheterocyclic scaffold has a carboethoxy substituent at C2 of the thiazole ring, aminolysis provides for effective diversification. A 50-member library of various 5-(thiazol-5-yl)-4,5-dihydroisoxazoles is reported. 相似文献