Novel synthesis of CP-734432, an EP4 agonist, using Sharpless asymmetric dihydroxylation
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- 作者：Sajiv K. Nair ; Jean J. Matthews ; Stephan J. Cripps ; Chunrong Ma ; Elena Z. Dovalsantos ; Alan W. Grubbs ; Neal W. Sach ; Wolter ten Hoeve ; Han Koster ; Erik J. Flahive ; Steven P. Tanis ; Matt Renner ; Jim va
- 刊名：Tetrahedron Letters
- 出版年：2010
- 出版时间：17 March 2010
- 年：2010
- 卷：51
- 期：11
- 页码：1451-1454
- 全文大小：456 K
文摘
A novel and efficient asymmetric route to CP-734432, a lactam analog of PGE2, that shows selective agonism against the EP4 receptor subtype, is reported herein. The key steps include a Heck coupling to introduce the aryl ring at C-16 and a highly diastereoselective Sharpless asymmetric dihydroxylation to set the C-15 center.