A Scalable Route to 5-Substituted 3-Isoxazolol Fibrinolysis Inhibitor AZD6564
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- 作者：S酶ren M. Andersen ; Martin Bollmark ; Robert Berg ; Christofer Fredriksson ; Staffan Karlsson ; Catarina Liljeholm ; Henrik S枚rensen
- 刊名：Organic Process Research & Development
- 出版年：2014
- 出版时间：August 15, 2014
- 年：2014
- 卷：18
- 期：8
- 页码：952-959
- 全文大小：352K
- ISSN：1520-586X
文摘
A practical and chromatography-free multikilogram synthesis of a 3-isoxazolol containing antifibrinolytic agent, AZD6564, has been developed in eight steps and 7% overall yield starting from methyl 2-chloroisonicotinate. Highlights in the synthesis are a Negishi coupling and an enzymatic resolution of a racemic ester.