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Published on: October 10, 2016
Highly C-selective difluoromethylation of β-ketoesters by using TMSCF2Br/lithium
Jiandong Wang1, Etsuko Tokunaga, Norio Shibata
1Department of Nanopharmaceutical Sciences, Nagoya Institute of Technology, Gokiso, Showa-ku, Nagoya 466-5888, Japan. nozshiba@nitech.ac.jp.
Abstract:
The highly C-selective difluoromethylation of β-ketoesters was achieved by combining TMSCF2Br/LiOH/N,N,N-trimethylhexadecan-1-ammonium bromide. Compared to other alkali metal salts or organic bases, lithium hydroxide, which served as a difluorocarbene activator from TMSCF2Br, was crucial in the control of high C/O regioselectivity.
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