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Copper-catalyzed Trifluoromethylation Of Unactivated Olefins.

A. T. Parsons, S. L. Buchwald
Published 2011 · Chemistry, Medicine

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The inclusion of fluorinated functional groups in small molecules has had a profound impact on the pharmaceutical, material, and agrochemical industries.[1, 2] In particular, the trifluoromethyl (CF3) substituent has emerged as an important functional group for the modulation of the physical properties in new pharmaceutical candidates as it has excellent metabolic stability, lipophilicity, and is electron-withdrawing in nature.[3] Myriad of fluorinated biologically active pharmaceutical compounds have been identified,[4] with an estimated 20% of drugs on the market containing fluorine.[1] On this basis, there has been a recent surge in the number of reports describing the formation of carbon–trifluoromethyl (C–CF3) bonds, demonstrating the continuing need for the development of efficient methods to incorporate these groups.
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