咪唑并[1, 2-a]吡啶甲酸衍生物的合成与表征

Synthesis and Characterization of Imidazo [1,2-a] pyridine carboxylic acid derivatives

摘要:

以3-三氟甲基-2-氨基吡啶为原料，通过NBS选择性溴化，再与溴代丙酮酸甲酯通过“一锅法”进行烷基化-环化反应，之后经选择性氯化、Suzuki偶联反应和水解，合成了咪唑并[1,2-a]吡啶甲酸衍生物。反应总收率达到36.5%。并对Suzuki偶联反应的催化剂和反应条件进行了探讨。

Abstract:

Versatile imidazo[1,2-a]pyridine carboxylic acid 1 could be prepared in five steps from commercially available 2-amino pyridine. Alkylation/cyclization with Methyl bromopyruvate, followed by selective chlorination with NCS and tandem Suzuki cross-coupling/hydrolysis, affords cyclopropane 1. The studies on the Suzuki cross-coupling/hydrolysis reaction conditions and catalysts were also carried out.