In recent years, deuterium incorporation into drugs and bioactive molecules have seen several beneficial advantages, including enhanced resistance to oxidation. Considering the importance of deuterium incorporation into drugs, direct regioselective C(sp3)-H deuteration of remote C-H bonds, especially of poorly reactive β C-H bonds, remains a challenge. Herein, a regioselective deuteration of inert C(sp3)-H bonds using inexpensive D2O has been developed. Unlike other deuterium labeling strategies, this mild method allows for highly regioselective β C-H deuteration, even amidst other weak C-H bonds.

β C-H deuteration of alcohols via imidate radicals

ACS Fall 2021

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