剑麻皂甙元资源利用的研究——Ⅰ.降血脂药去脂舒的合成

Studies on the Utilization of Tigogenin Ⅰ. Synthesis of Quzhishu-- A Hypolipemic Agent

摘要: 本文报道了利用国产资源剑麻皂甙元制备降血脂药去脂舒的合成方法。为了适应工业生产,改进了合成中间体17β甲基17β,3β二羟基-5β雄甾烷(Ⅱ)与17β甲基17β羟基-5γ雄甾酮-3(Ⅲ)的反应条件,改变了合成17γ甲基17β羟基-5γ雄甾-2酮肟-3酮(Ⅳ)的工艺路线,从而简化了生产工艺、缩短了反应周期、提高了收率。现已被国内药厂采用。

Abstract: This article describes a method of synthesis of Qu-zhi-shu (l7α- methyl-17β-hydroxy-5α-androstano (2,3-c) furazan) a hypolipemic agent from the Tigogenin.In order to meet the requirements of industrial production, the synthetic conditions of the intermediates,l7α- methyl-17β, 3β -dihydroxyl -5αandrostane (Ⅱ)and l7α- methyl-17β-hydroxy-5α-androstan-3 one(Ⅲ) have been modified, and the productive route of another intermediate, l7α- methyl-17β-hydroxy-2-hydroximino-Androstan 3-one (Ⅳ) has also been partially altered, so as to simplify the productive process and increase the yield. This method is being used by Wuxian pharmaceutical factory.