2-氨基-3-三氟甲基苯甲酸的合成

2-氨基-3-三氟甲基苯甲酸为一个重要的药物合成中间体,对其合成方法进行了研究.以2-三氟甲基苯胺、水合氯醛、盐酸羟胺为原料,合成2-氨基的衍生物,然后在浓硫酸中转化为邻位二羰基衍生物,最后在氢氧化钠水溶液中用双氧水氧化得到2-氨基-3-三氟甲基苯甲酸.以2-三氟甲基苯胺计,2-氨基-3-三氟甲基苯甲酸的总收率为53.6%.所得的产物结构经元素分析、红外光谱、核磁共振谱所证实.该合成方法操作简便,收率较高,该方法所有合成步骤均为水相反应,易于工业化.

Synthesis of 2 - Amino - 3 - (Trifluoromethyl) - Benzoic Acid

The synthesis of 2-amino-3-(trifluoromethyl)-benzoic acid, an important intermediate for the pharmaceutical synthesis, is reported in this paper.Substituted trifluoromethyl aniline is synthesized from 2-(trifluoromethyl) aniline, chloral hydrate and hydroxylamine hydrochloride. 3-(trifluoromethyl)isatin is prepared from substituted trifluoromethyl aniline in concentrated sulphuric acid. Finally, 2-amino-3-(trifluromethyl)-benzoic acid is derived by reacting 3-((trifluoromethyl)-isatin with hydrogen peroxide in the presence of sodium hydroxide. Starting from 2-(trifluoromethyl) aniline , 2-amino-3-(trifluoromethyl)-benzoic acid is synthesized with a yield of 53.6%.Structures of the resultants are identified by 1HNMR, IR and elemental analysis. The preparation is made in water and this method is easily applied in the industry.