卡托普利合成方法的改进

An Improved Synthetic Method of Captopril

甲基丙烯酸与溴化氢反应得到３－溴－２－甲基丙酸，后者经用氯化亚砜氯化、与Ｌ－脯氨酸缩合得到缩合酸．缩合酸再经分拆、巯基化得到卡托普利．

An improved synthetic method for Captopril(Ⅰ)when using methacrylic acid as the starting material is described in this paper.Treatment of methacrylic acid(Ⅱ) with hydrogen bromide gave 3 bromo 2 methylpropanoic acid(Ⅲ) which underwent chlorination with thionyl chloride,condensation with L proline gave N (R.S 3 bromo 2 methylpropanoyl) L proline(Ⅴ).Ⅴ was resoluted into optically pure stereo isomer,which was treated with sodium trithiocarbonate to give Captopril(Ⅰ).