盐酸阿考替胺三水合物的合成  

Synthesis of Acotiamide Hydrochloride Trihydrate

作　　者：白晓光[1] 杨志衡 李子强[1] 王菊仙[1] 王玉成[1] 

机构地区：[1]中国医学科学院,北京协和医学院医药生物技术研究所,北京100050

出　　处：《中国医药工业杂志》2015年第3期230-232,共3页Chinese Journal of Pharmaceuticals

摘　　要：2,4,5-三甲氧基苯甲酸经氯化铝脱甲基得2-羟基-4,5-二甲氧基苯甲酸,与亚磷酸三苯酯反应生成2-羟基-4,5-二甲氧基苯甲酸苯酯,再与2-氨基噻唑-4-甲酸甲酯缩合得2-[(2-羟基-4,5-二甲氧基苯甲酰基)氨基]噻唑-4-羧酸甲酯,然后与N,N-二异丙基乙二胺酰化、与盐酸成盐、精制得盐酸阿考替胺三水合物,总收率75%。Acotiamide hydrochloride trihydrate was synthesized from 2,4,5-trimethoxybenzoic acid by demethylation with aluminium chloride to give 2-hydroxy-4,5-dimethoxybenzoic acid, which was subjected to esterification with triphenyl phosphite and condensation with methyl 2-aminothiazole-4-carboxylate, and then acylation with N,N-diisopropylethane- 1,2-diamine, salt formation and recrystalization with an overall yield of 75 %.

关 键 词：阿考替胺 功能性消化不良 合成 

分 类 号：R975.1[医药卫生—药品]