The incorporation of fluorine into bioactive molecules is of special interest to the pharmaceutical and agrochemical industries due to the ability of fluorine to increase metabolic stability, lipophilicity and bioavailability of these compounds. Approximately 20-30% of pharmaceutical and more than 50% of new agrochemical compounds on the market contain fluorine. Major classes of organofluorine compounds found in these bioactive molecules include aryl fluorides, trifluoromethyl-, and difluoromethyl groups. Here, we present the development of an efficient transition metal-catalyzed protocol for the incorporation of a difluoromethyl group using a commercially available electrophilic difluoromethylation reagent.

Development of new difluormethylation reactions

2019 Fall National Meeting

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