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PROCESS FOR THE PREPARATION OF OSELTAMIVIR AND METHYL 3-EPI-SHIKIMATE

机译:奥司他韦和3-EPI-Shikimate甲酯的制备方法

摘要

The present invention discloses high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol. The process features incorporation of chirality using sharpless asymmetric epoxidation (AE) and diastereoselective Barbier allylation and construction of cyclohexene carboxylic acid ester core through a ring closing metathesis (RCM) reaction. Further also disclosed herein is synthesis of (−)-methyl 3-epi-shikimate.
机译:本发明公开了由容易获得的起始原料顺式1,4-丁烯二醇合成奥瑟他韦的高产率对映选择性方法。该方法的特点是采用无尖锐的不对称环氧化(AE)和非对映选择性的Barbier烯丙基化手性,并通过闭环复分解(RCM)反应构建环己烯羧酸酯核。本文还还公开了3-(epi-shikimate)-(-)-甲基的合成。

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