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Cyclic Anti-Azacarboxylation of 2-Alkynylanilines with Carbon Dioxide

Bukeyan Miao, Suhua Li, Gen Li and Shengming Ma*

*Shanghai Key Laboratory of Green Chemistry and Chemical Process, Department of Chemistry, East China Normal University, 3663 North Zhongshan Lu, Shanghai 200062, P. R. China, Email:

B. Miao, S. Li, G. Li, S. Ma, Org. Lett., 2016, 18, 2556-2559.

DOI: 10.1021/acs.orglett.6b00884 (free Supporting Information)


Direct anti-azacarboxylation of 2-alkynylanilines with CO2 mediated by ZnEt2 affords indole-3-carboxylic acids efficiently under 1 atm of CO2. The availability of starting materials and tolerance of various functional groups provide vast opportunities for the efficient construction of diversified libraries for bioactive compounds.

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ID: J54-Y2016