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

页码：408 / 413

页数：6

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