Improved synthesis of the PAR-1 thrombin receptor antagonist RWJ-58259

被引：0
作者：
Valdivielso, Angel M. [1 ]
Teresa Garcia-Lopez, M. [1 ]
Herranz, Rosario [1 ]
机构：
[1] CSIC, Inst Quim Med, E-28006 Madrid, Spain
来源：
ARKIVOC | 2008年
关键词：
Peptidomimetics; heterocycles; alkylation; ureas; protease-activated receptor antagonists;
D O I：
暂无
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A significant improvement on the synthesis of the PAR-1 antagonist RWJ-58259 is described, which involves a base-related two-fold yield increase in the indazole N-alkylation, and an easier purification and a nine-fold yield increase in the urea formation, by using triphosgene/propylene oxide as urea coupling traceless reagents.
引用
收藏
页码：287 / 294
页数：8
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