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

作者信息

Pontillo Joseph, Chen Chen

机构信息

Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.

出版信息

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1407-11. doi: 10.1016/j.bmcl.2005.01.009.

DOI:10.1016/j.bmcl.2005.01.009
PMID:15713397
Abstract

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).

摘要

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