Difluoromethylation of aryl and vinyl iodides

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United States of America Patent

PATENT NO 9475756
APP PUB NO 20150045580A1
SERIAL NO

14382991

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Selectively fluorinated molecules are important as materials, pharmaceuticals, and agrochemicals, but their synthesis by simple, mild, laboratory methods is challenging. We report a straightforward method for the cross-coupling of a difluoromethyl group with readily available reagents to form difluoromethylarenes. The reaction of electron-neutral, electron rich, and sterically hindered aryl and vinyl iodides with the combination of CuI, CsF and TMSCF2H leads to the formation of difluoromethylarenes in high yield with good functional group compatibility. This transformation is surprising, in part, because of the prior observation of the instability of CuCF2H.

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THE REGENTS OF THE UNIVERSITY OF CALIFORNIA1111 FRANKLIN STREET OAKLAND CA 94607-5200

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Fier, Patrick Berkeley, US 7 7
Hartwig, John Berkeley, US 5 7

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