The application of high-throughput synthesis and purification to the preparation of ethanolamines

被引:42
作者
Shuker, AJ
Siegel, MG
Matthews, DP
Weigel, LO
机构
[1] ELI LILLY & CO,LILLY RES LABS,ENDOCRINE RES,INDIANAPOLIS,IN 46285
[2] ELI LILLY & CO,LILLY RES LABS,CHEM PROC R&D,INDIANAPOLIS,IN 46285
关键词
D O I
10.1016/S0040-4039(97)01421-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A 48 compound library of structurally diverse ethanolamines was prepared using a parallel synthesis approach. The synthetic paradigm employed a solution phase epoxide-opening reaction followed by rapid purification by ion exchange chromatography to yield products with near-analytical purity. An array of epoxides and primary amines, arranged in an 8x6 matrix, were reacted in the presence of an in situ silylating agent to form 48 individual compounds with an average yield of 75% and an average purity of 92.3%. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:6149 / 6152
页数:4
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