A Practical Synthesis of 2-Aroylindoles from N-(2-Formylphenyl)trifluoroacetamides in PEG-400

Yu Zhao, Deyao Li, Liwen Zhao, Jiancun Zhang*

*Guangzhou Institute of Biomedicine and Health, CAS, 190 Kai Yuan Avenue, Science Park, Guangzhou 510530, P. R. of China, Email: zhang_jiancungibh.ac.cn

Y. Zhao, D. Li, L. Zhao, J. Zhang, Synthesis, 2011, 873-880.

DOI: 10.1055/s-0030-1258445

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Abstract

The reaction of easily accessible N-(2-formylphenyl)trifluoroacetamides and α-bromoacetophenones in the presence of K₂CO₃ enables a one-pot and environmentally benign approach to the synthesis of highly functionalized 3-unsubstituted 2-aroylindoles. PEG-400 is an efficient and reusable solvent in this process.

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Key Words

2-aroylindoles, indoles, PEG-400, N-(2-formylphenyl)trifluoroacetamides, heterocycles, cyclization, Green Chemistry

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ID: J66-Y2011-0670