（R）-2-[4-甲氧基-3-（3-甲氧基丙氧基）苄基]-3-甲基丁酸的制备改进

本文以异香草醛为原料经过5步反应合成了Aliskiren的一个重要中间体——（R）-2-[4-甲氧基-3-（3-甲氧基丙氧基）苄基]-3-甲基丁酸。醚化中采用超声波反应，缩短了反应时间，提高了产率。所需手性中心由（R）-3-异戊酰基-4-苄基-2-噁唑烷酮诱导产生，针对去除诱导剂时需断裂环外酰胺键，通常会先引起分子中的酯键断裂，因而很难将诱导剂断裂下来，实验采用氢过氧化锂（LiOOH）高选择性地断裂环外酰胺键，实验还选用钙盐沉淀法纯化目标产物，均取得良好的效果。

Improving synthetic method of (R)-2-(4-methoxy-3-(3-methoxypropoxy)benzyl)-3-methylbutanoic acid

In this paper, the important intermediates of Aliskiren,(R)-2-(4-methoxy-3-(3-methoxypropoxy) benzyl)-3-methylbutanoic acid was synthesized by five step reaction using the isovanillin as raw material. The ultrasonic reaction was applied to the etherification that reduced the reaction time and raised the yield. The chiral center was induced by the(R)-3-isovaleryl-4-benzyl-oxazolidin-2-one. As the removal of chiral auxiliary,exocyclic amide bond was needed to break,it usually resulted in the ester bond breaki...