Synthesis of 2-(Trifluoromethyl)indoles via Domino Trifluoromethylation/Cyclization of 2-Alkynylanilines
Yibin Ye, Kelvin Pak Shing Cheung, Lisi He and Gavin Chit Tsui*
*Department of Chemistry, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, Email: gctsuicuhk.edu.hk
Y. Ye, K. P. S. Cheung, L. He, G. C. Tsui, Org. Lett., 2018, 20, 1676-1679.
DOI: 10.1021/acs.orglett.8b00509 (free Supporting Information)
The use of the well-established fluoroform-derived CuCF3 reagent enables the synthesis of 2-(trifluoromethyl)indoles from easily accessible 2-alkynylanilines via a domino trifluoromethylation/cyclization strategy. 3-formyl-2-(trifluoromethyl)indoles can also be synthesized, which are useful intermediates for the preparation of trifluoromethylated drug analogues.
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