Fully Automated Continuous Flow Synthesis of Highly Functionalized Imidazo[1,2-a] Heterocycles

被引：84

作者：

Herath, Ananda ^{[1
]}

Dahl, Russell ^{[1
]}

Cosford, Nicholas D. P. ^{[1
]}

机构：

[1] Burnham Inst Med Res, Program Apoptosis & Cell Death Res & Conrad Preby, Ctr Chem Genom, La Jolla, CA 92037 USA

来源：

ORGANIC LETTERS | 2010年 / 12卷 / 03期

基金：

美国国家卫生研究院;

关键词：

MULTISTEP SYNTHESIS; ORGANIC-SYNTHESIS; RAPID CONSTRUCTION; CHEMICAL SPACE; EFFICIENT; CHEMISTRY; REACTOR; MICROREACTOR; DERIVATIVES; TECHNOLOGY;

D O I：

10.1021/ol902433a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The first continuous flow synthesis of imidazo[1,2-a]pyridine-2-carboxylic acids directly from 2-aminopyridines and bromopyruvic acid has been developed, representing a significant advance over the corresponding in-flask method. The process was applied to the multistep synthesis of imidazo[1,2-a]pyridine-2-carboxamides, including a Mur ligase inhibitor, using a two microreactor, multistep continuous flow process without isolation of intermediates.

引用

收藏

页码：412 / 415

页数：4

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