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One-Pot Synthesis of Indole-3-acetic Acid Derivatives through the Cascade Tsuji-Trost Reaction and Heck Coupling

Dongsheng Chen, Yuanyuan Chen, Zhilong Ma, Lei Zou, Jianqi Li* and Yu Liu*

*Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 201203, People's Republic of China, Email:,

D. Chen. Y. Chen, Z. Ma, L. Zou, J. Li, Y. Liu, J. Org. Chem., 2018, 83, 6805-6814.

DOI: 10.1021/acs.joc.8b01056

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The use of a Pd(OAc)2/P(o-tol)3/DIPEA system enables a practical cascade Tsuji-Trost reaction/Heck coupling of N-Ts o-bromoanilines with 4-acetoxy-2-butenonic acid derivatives to provide various substituted indole/azaindole-3-acetic acid derivatives.

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Key Words


ID: J42-Y2018