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A series of β-N-(4-methoxybenzoyl)- and β-N-(3-nitrobenzoyl)hydrazides of 4-aryl-2-hydroxy-4-oxo-2- butenoic (aroylpyruvic) acids was obtained with 52 – 88% yields using the reaction of decyclization of 5-aryl-2,3-dihydrofuran-2,3-diones by hydrazides of 4-methoxybenzoic and 3-nitrobenzoic acid hydrazides in dioxane. The synthesized compounds were characterized and tested for antibacterial activity.__________Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 3, pp. 21 – 22, March, 2005.  相似文献   

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Pharmaceutical Chemistry Journal - Reactions of 4-(4-bromoacetylphenyl)-3-hydroxy-2H-chromen-2-one with Py, 4-methylpyridine, quinoline, and benzo[f]quinoline produced quaternary salts; with...  相似文献   

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Pharmaceutical Chemistry Journal - Aseries of previously unreported N-aryl-7-hydroxy-2-imino-2H-chromene-3-carboxamides were synthesized via the reaction of 2,4-dihydroxybenzaldehyde with...  相似文献   

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2—羟基—3—氨基—4—苯丁酸的合成   总被引:3,自引:1,他引:3  
2-羟基 - 3-氨基 - 4-苯丁酸 (1 )是制备二肽免疫增强剂类抗癌新药乌苯美司的关键中间体 ,有多种合成方法 ,如 α-氨基苯乙酮法 [1]、α-氨基苯丙醛法 [2 ]、α-氨基苯丁腈法[3] 、苯丁烯酸甲酯法 [4 ] 、苯丙氨酸法 [5]和苹果酸二乙酯法 [6]等。以上各法均存在不同缺点 ,如α-氨基苯乙酮法 ,总收率不到 1 0 % ;α-氨基苯丙醛法和α-氨基苯丁腈法 ,均用剧毒氰化钾(钠 ) ;苯丁烯酸甲酯法用爆炸性的过氧化物 ;苯丙氨酸法合成步骤长 ,且用氢化铝锂和氰化钠等试剂 ;苹果酸二乙酯法中的烃化反应需在 - 78℃的低温下进行。上述各法均不适合工业化…  相似文献   

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Preclinical Research
A series pf novel (7S, 11R)—substituted diphenyl‐2,4,8,10‐tetraazaspiro [5.5] undecane‐3‐thio‐1,5,9‐triones 4a‐j and (7S,11R)‐substituted diphenyl‐2,4,8,10‐tetraazaspiro[5.5] undecane‐3‐thio‐1,5 dione, 9‐thiones 5a‐j were prepared using substituted aldehydes and urea/thiourea in the presence of thiobarbituric acid under solvent free, thermal and microwave conditions catalyzed by ecofriendly K‐10 clay. The antibacterial potency of these compounds in vitro on the gram negative strains Escherichia coli and Pseudomonas aeruginosa and gram positive strains Staphyllococcus aureus and Staphylococcus epidermidis was evaluated.  相似文献   

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Pharmaceutical Chemistry Journal - The synthesis and anticonvulsant activity of new coumarin derivatives are reported. N-(3-Nitrocoumarin-4-yl)-4-aminobutyric acid (1a) at doses of 60 and 80 mg/kg...  相似文献   

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