盐酸坦索罗辛的合成

Synthesis of Tamsulosin Hydrochloride

以4-甲氧基苯丙酮为原料,依次经过(R)-苯乙胺诱导的还原胺化、氯乙酰化、氯磺化和氨化反应制得N-(R)-[2-(4-甲氧基-3-氨基磺酰基苯基)-1-甲基乙基]-N-(R)-(1-苯乙基)-氯乙酰胺,再经烷基化、还原和催化脱苄等反应制得盐酸坦索罗辛,总收率约15%。

Tamsulosin hydrochloride was synthesized from 4-methoxyphenylacetone by reductive amination with chiral induction of （R）-phenethylamine, chloracetylation, chlorosulfonation and amination to give N-（R）- [2-（4- methoxy-3-aminosulfonylphenyl） - 1-methylethyl] -N- （R） - （1-phenylethyl） -chloroacetamide, which was subjected to alkylation, reduction and catalytic debenzylation with an overall yield of 15 %.