Development of a Scalable Synthesis of GSK183390A, a PPAR α/γ Agonist
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- 作者：Lynette M. Oh ; Huan Wang ; Susan C. Shilcrat ; Robert E. Herrmann ; Daniel B. Patience ; P. Grant Spoors ; Joseph Sisko
- 刊名：Organic Process Research & Development
- 出版年：2007
- 出版时间：November 2007
- 年：2007
- 卷：11
- 期：6
- 页码：1032 - 1042
- 全文大小：1004K
- 年卷期：v.11,no.6(November 2007)
- ISSN：1520-586X
文摘
A scalable synthesis of GSK183390A, a PPAR α/γ agonist, is described. This synthesis is highlighted by (1) a regioselective formal 1,3-dipolar cycloaddition reaction between an enamine and a nitrile imine dipole to form a 1,3,5-trisubstituted pyrazole and (2) a regioselective amidomethylation of an ο-cresol derivative using 2-chloro-N-hydroxymethylacetamide.