Solid-phase synthesis of a tyrphostin ether library

被引:20
|
作者
Guo, GH [1 ]
Arvanitis, EA [1 ]
Pottorf, RS [1 ]
Player, MR [1 ]
机构
[1] 3 Dimens Pharmaceut Inc, Cranbury, NJ 08512 USA
来源
JOURNAL OF COMBINATORIAL CHEMISTRY | 2003年 / 5卷 / 04期
关键词
D O I
10.1021/cc030003i
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The solid-phase synthesis of a 4500-member (30 x 15 x 10) tyrphostin library is demonstrated utilizing the Irori-directed sorting system. Fmoc-protected PL-Rink resin was used as the solid support. After Fmoc-deprotection, aryl aldehydes were attached to the resin through reductive amination. Acylation of the resulting secondary amines with cyanoacetic acid was followed by a Knoevenagel condensation with phenolic aldehydes. Mitsunobu coupling of primary alcohols to the resin-bound phenols yielded the final library of compounds 1.
引用
收藏
页码:408 / 413
页数:6
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