Efficient solution phase parallel synthesis of norstatine analogs

被引:11
|
作者
Voronkov, MV
Gontcharov, AV
Wang, ZM
Richardson, PF
Kolb, HC
机构
[1] Lexicon Pharmaceut, Med Chem, Princeton, NJ 08540 USA
[2] Wyeth Res, Pearl River, NY 10965 USA
[3] Rhodia Chirex, Boston, MA 02129 USA
[4] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
关键词
epoxide; nitrile; norstatine; solution phase combinatorial chemistry;
D O I
10.1016/j.tet.2004.07.085
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The reaction of glycidic amides with various functionalized nitriles to afford norstatine analogs in a regio- and diastereoselective fashion (43-99% yield) is described. Utilizing this chemistry, a 20 membered solution phase library was prepared in two steps featuring three points of diversity. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:9043 / 9048
页数:6
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