抗精神分裂症药瑞莫必利的合成

Synthesis of Antischizophrenic Remoxipride

摘要: 以２，６－二羟基苯乙酮为原料，经甲基化、氧化、溴代以及与拆分得到的手性原料Ｓ（－）－２－氨甲基－Ｎ－乙基四氢吡咯的酰化等反应合成了瑞莫必利，总收率５４％（以２，６－二羟基苯乙酮计）。

Abstract: Starting from 2,6 dihydroxyacetophenone, and undergoing methylation, oxidation, bromination and then amidation with S ( ) 2 aminomethyl 1 ethylpyrrolidine which was prepared from the raceme with D ( ) tartaric acid as resolving agent, we syn