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 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第3期230-232,共3页
Chinese Journal of Pharmaceuticals
