Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-clpyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists

被引：16

作者：

Pontillo, J ^{[1
]}

Chen, C ^{[1
]}

机构：

[1] Neurocine Biosci Inc, Dept Med Chem, San Diego, CA 92130 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期

关键词：

D O I：

10.1016/j.bmcl.2005.01.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Treatment of various 2-methyl oxazolines or thiazolines with chlorocarbonyl isocyanate gives the corresponding bicyclic oxazolino- or thiazolino[3,2-c]pyrimidin-5,7-dione derivatives in very good yield. This reaction has been applied to the rapid syntheses of human gonadotropin-releasing hormone (hGnRH) receptor antagonists for SAR study, resulting in 13e with binding affinity in the low nanomolar range (4.5 nM). (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1407 / 1411

页数：5

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