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Paper | Regular issue | Vol 91, No. 11, 2015, pp.2087-2096
Published online, 27th October, 2015
DOI: 10.3987/COM-15-13299
Microwave Assisted Synthesis of Disubstituted Imidazo[1,2-a]pyridine-3-carboxylic Acid Esters

Lin-hu Li, Zhao-yang Wu, Zhuo-rong Li, Ming-liang Liu,* Hui-yuan Guo, and Qiu-rong Zhang*

*Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, China


A novel and efficient synthetic method leveraging microwave-assisted organic synthesis (MAOS) to prepare disubstituted imidazo[1,2-a]- pyridine-3-carboxylic acid esters (IPCEs) (3a-z), the key intermediates for a class of novel anti-tuberculosis agents, is reported. Under microwave heating at 120 °C for 20 or 30 min, the condensations of 2-aminopyridines (1a-k) and ethyl 2-halogenated acetoacetates (2a-d) were conveniently performed in ethanol with acceptable yields.