Program in Apoptosis and Cell Death Research and Conrad Prebys Center for Chemical Genomics, Burnham Institute for Medical Research, 10901 North Torrey Pines Road, La Jolla, California 92037, USA.
Org Lett. 2010 Feb 5;12(3):412-5. doi: 10.1021/ol902433a.
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.
已开发出一种直接从 2-氨基吡啶和溴丙酮酸合成咪唑并[1,2-a]吡啶-2-羧酸的连续流合成方法,这是对相应的瓶内方法的重大改进。该方法应用于咪唑并[1,2-a]吡啶-2-羧酰胺的多步合成,包括 Mur 连接酶抑制剂,使用两个微反应器,多步连续流过程,无需分离中间体。