A bench-stable reagent for C-4 selective deuteriodifluoromethylation of azines |
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Institution: | 1. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;2. Research Center of Analysis and Test, School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237, China |
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Abstract: | Deuteriodifluoromethyl (CF2D) is a challenging and important functional group due to difficult deuterium incorporation and lack of effective precursor reagents. Herein, we report a bench-stable reagent, deuteriodifluoromethyl phosphine (DDFP) from cheap deuterium source for selectivity deuteriodifluoromethylation of azines with a high deuterium incorporation yield. The late-stage modification of complex molecules further confirmed the potential of this reagent for practical applications. We expect that our reagent to find applications in synthesis of isotope-labelled molecules of interests for drug-discovery and related ilucidation of mechanism of action. |
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