Solid-phase synthesis of a tyrphostin ether library |
| |
Authors: | Guo Guihua Arvanitis Elena A Pottorf Richard S Player Mark R |
| |
Affiliation: | 3-Dimensional Pharmaceuticals, Inc, 8 Clarke Drive, Cranbury, New Jersey 08512, USA. |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|