Preparation of Heteroaryloxetanes and Heteroarylazetidines by Use of a Minisci Reaction

被引：82

作者：

Duncton, Matthew A. J. ^{[1
]}

Estiarte, M. Angels ^{[1
]}

Johnson, Russell J. ^{[1
]}

Cox, Matthew ^{[1
]}

O'Mahony, Donogh J. R. ^{[1
]}

Edwards, William T. ^{[1
]}

Kelly, Michael G. ^{[1
]}

机构：

[1] Evotec USA, San Francisco, CA 94080 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2009年 / 74卷 / 16期

关键词：

FREE-RADICAL REACTIONS; PROTONATED HETEROAROMATIC BASES; TRIVALENT IODINE COMPOUNDS; HORMONE TRH ANALOGS; O-SULFONIC ACID; HOMOLYTIC ACYLATION; NUCLEOPHILIC CHARACTER; ANTITUMOR-ACTIVITY; CARBOXYLIC-ACIDS; ACYL RADICALS;

D O I：

10.1021/jo9010624

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Introduction of oxetan-3-yl and azetidin-3-yl groups into heteroaromatic bases was achieved by using a radical addition method (Minisci reaction). To demonstrate utility. the process was used to introduce an oxetane Or azetidine into heteroaromatic systems that have found important uses in the drug discovery industry, such as the marketed EGFR inhibitor geftinib, a quinolinecarbonitrile Src tyrosine kinase inhibitor, and the antimalarial hydroquinine.

引用

页码：6354 / 6357

页数：4

共 81 条

[31] High-throughput kinase profiling as a platform for drug discovery [J].