文献类型：专利

英文题名：Preparation of N-(5-nitro-2-thiazolyl) benzamide derivative involves reacting 2-azyl-5-nitro thiazole, acid-binder, and tetrahydrofuran or anhydrous tetrahydrofuran, stirring, and dripping mixture containing benzoyl halogen derivative

作者：CHANG W;GAO P;YAN J;ZHUO C

机构：[1]UNIV EAST CHINA SCI & TECHNOLOGY

申请号：CN101704798-A

申请日：2009-10-30

公开日：2010-05-12

语种：英文

收录：DERWENT

摘要：NOVELTY - A N-(5-nitro-2-thiazolyl) benzamide derivative (I) is prepared by reacting 2-azyl-5-nitro thiazole, acid-binder, and tetrahydrofuran or anhydrous tetrahydrofuran, and stirring; dripping mixture containing benzoyl halogen derivative (II) and tetrahydrofuran or anhydrous tetrahydrofuran, stirring, and pouring into ice and/or water; and separating precipitate, filtering, and refining solid. USE - Method of preparing N-(5-nitro-2-thiazolyl) benzamide derivative (claimed). ADVANTAGE - The method has low preparation cost, and simple synthesis route. DETAILED DESCRIPTION - Preparation of N-(5-nitro-2-thiazolyl) benzamide derivative of formula (I) involves reacting 2-azyl-5-nitro thiazole, acid-binder, and tetrahydrofuran or anhydrous tetrahydrofuran, and stirring; dripping mixture containing benzoyl halogen derivative of formula (II) and tetrahydrofuran or anhydrous tetrahydrofuran at - 5-0 degrees C, stirring at 40-50 degrees C for 3-5 hours, and pouring into ice and/or water having pH value of 2-6 (preferably 2-3); and separating precipitate, filtering, and refining solid. The mole ratio of 2-azyl-5-nitro thiazole to acid-binder is 1:(1.5-2.5); and 2-azyl-5-nitro thiazole to benzoyl halogen derivative (II) is 1:(1-1.5). The acid-binder is inorganic or organic alkali, or triethylamine. R1-R5=-OCOCH3, -OH or H; and X=Cl, Br or I. Provided that: (1) anhydrous tetrahydrofuran is used as reaction solvent when R1 is -OCOCH3, R2-R5 are H, and X is Cl; and (2) tetrahydrofuran is used as reaction solvent when R1 is -OH, R2-R5 are H, and X is Cl.