盐酸川丁特罗中间体3-氯-4-氨基-5-三氟甲基苯乙酮的合成

The synthesis of 4-amino-3-chloro-5-trifluoromethylacetophen-one,the intermediate of trandinterol hydrochloride

目的合成盐酸川丁特罗的重要中间体3-氯-4-氨基-5-三氟甲基苯乙酮。方法以邻-三氟甲基苯胺为起始原料,经碘代、酰化、氰基取代、水解、取代、氯代和烃化7步反应得到盐酸川丁特罗的重要中间体。结果与结论目标化合物的结构经1H-NMR和MS确证,总收率为8.9%。该合成工艺操作简便,适合工业化生产。

Aim To synthesize the key intermediate of tradinterol hydrochloride 4-amino-3-chloro-5-trifluoromethylacetophenone.Methods The intermediate was prepared from 2-trifluoromethyl-aniline through 7 step reactions that include iodination,acylation,cyano-substitution,hydrolysis reaction,substitution,chlorination,alkylation.Results and conclusion The structure of 4-amino-3-chloro-5-trifluoromethylacetophenone was confirmed by 1H-NMR and MS,and the overall yield was 8.9%.This synthetic process is easy to scale up for its convenient operation.