无催化剂、C-3 位官能化的咪唑并[1,2-a]吡啶，为药物研发工作迅速开辟新的化学空间。
Catalyst free, C-3 functionalization of imidazo[1,2-a]pyridines to rapidly access new chemical space for drug discovery efforts.
机构信息
Department of Pharmaceutical Sciences, University of Arkansas for Medical Sciences, Little Rock, 72205, USA.
出版信息
Chem Commun (Camb). 2018 Nov 15;54(92):12954-12957. doi: 10.1039/c8cc07063f.
Abstract
Multicomponent reactions (MCRs) are robust tools for the rapid synthesis of complex, small molecule libraries for use in drug discovery and development. By utilizing MCR chemistry, we developed a protocol to functionalize the C-3 position of imidazo[1,2-a]pyridine through a three component, decarboxylation reaction involving imidazo[1,2-a]pyridine, glyoxalic acid, and boronic acid.
摘要
多组分反应（MCRs）是快速合成用于药物发现和开发的复杂小分子库的强大工具。通过利用 MCR 化学，我们开发了一种通过涉及咪唑并[1,2-a]吡啶、乙二醛酸和硼酸的三组分脱羧反应在咪唑并[1,2-a]吡啶的 C-3 位置进行功能化的方案。
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