A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists

被引：14
作者：
Guo, ZQ
Wu, DP
Zhu, YF
Tucci, FC
Pontillo, J
Saunders, J
Xie, Q
Struthers, RS
Chen, C
机构：
[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92130 USA
[2] Neurocrine Biosci Inc, Dept Endocrinol, San Diego, CA 92130 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 03期
关键词：
GnRH; antagonist; triazinetrione;
D O I：
10.1016/j.bmcl.2004.11.026
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A convenient one-pot synthetic route was developed for the preparation of asymmetric 1,3-dialkyl-1,3,5-triazine-2,4,6-triones from readily available alkyl- or aryl-isocyanates, primary amines and N-chlorocarbonyl isocyanate in excellent yields. Subsequent alkylation with N-protected amino alcohols afforded the desired 1, 3,5 -triazine-2,4,6-triones in good yields. This methodology was applied to the synthesis of a chemical library acting as antagonists of the hGnRH receptor. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：693 / 698
页数：6
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