Synthesis of (−)-Paroxetine via Enantioselective Phase-Transfer Catalytic Monoalkylation of Malonamide Ester

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• 作者：Mi-hyun Kim ; Yohan Park ; Byeong-Seon Jeong ; Hyeung-geun Park ; Sang-sup Jew
• 刊名：Organic Letters
• 出版年：2010
• 出版时间：June 18, 2010
• 年：2010
• 卷：12
• 期：12
• 页码：2826-2829
• 全文大小：174K
• 年卷期：v.12,no.12(June 18, 2010)
• ISSN：1523-7052

文摘

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.