摘要
4-乙酰胺基-2-甲氧基苯甲酸甲酯经浓硫酸磺化、水解、氯化、还原后与溴乙烷反应,再水解得到3-乙基磺酰基-4-氨基-6-甲氧基苯甲酸,最后与1-乙基-2-氨甲基吡咯烷在三乙胺和氯甲酸乙酯作用下缩合制得抗精神分裂症药氨磺必利,总收率约61%。
Amisulpride, a novel atypical antipsychotic drug, was synthesized from methyl 4-acetamido-2- methoxybenzoate by sulfonation with sulfuric acid, hydrolysis, chlorination, reduction, reaction with bromoethane and then hydrolysis to give 3-ethylsulfonyl-4-amino-6-methoxybenzoic acid, which was subjected to condensation with 1-ethyl-2- (aminomethyl) pyrrolidine in the presence of triethylamine and ethyl chloroformate. The overall yield was about 61%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2011年第11期801-803,共3页
Chinese Journal of Pharmaceuticals