通过马来酰胺酯的对映选择性相转移催化单烷基化反应合成（-）-帕罗西汀。
Synthesis of (-)-paroxetine via enantioselective phase-transfer catalytic monoalkylation of malonamide ester.
机构信息
Research Institute of Pharmaceutical Science and College of Pharmacy, Seoul National University, Seoul 151-742, Korea.
出版信息
Org Lett. 2010 Jun 18;12(12):2826-9. doi: 10.1021/ol100928v.
PMID:20499863
Abstract
A new enantioselective synthetic method of (-)-paroxetine is reported. (-)-Paroxetine could be obtained in 15 steps (95% ee and 9.1% overall yield) from N,N-bis(p-methoxyphenyl)malonamide tert-butyl ester via the enantioselective phase-transfer catalytic alkylation and the diastereoselective Michael addition as the key steps.
摘要
报道了一种 (-)-帕罗西汀的新型对映选择性合成方法。(-)-帕罗西汀可由 N,N-双（对甲氧基苯基）丙二酰胺叔丁酯经对映选择性相转移催化烷基化和非对映选择性迈克尔加成反应作为关键步骤，以 15 步（95%ee 和 9.1%总收率）得到。
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