Author/Authors :
Yun-Fei Zhu، نويسنده , , Keith Wilcoxen، نويسنده , , John Saunders، نويسنده , , Zhiqiang Guo، نويسنده , , Yinghong Gao، نويسنده , , Patrick J. Connors Jr.، نويسنده , , Timothy D. Gross، نويسنده , , Fabio C. Tucci، نويسنده , , R. Scott Struthers، نويسنده , , Greg J. Reinhart، نويسنده , , Qiu Xie، نويسنده , , Chen Chen، نويسنده ,
Abstract :
In the process of developing GnRH receptor antagonists, a novel base-catalyzed cyclization of compounds 5a–b was discovered, which led to the formation of the 2-aryl pyrrolo[1,2-a]pyrimid-7-one core stuctures 6a–b. These intermediates were further modified at positions 1, 2, 4 and 6 to afford a series of potent GnRH antagonists with low nanomolar Ki values.
