Remote Site?Selective Radical C(sp ³ )?H Monodeuteration of Amides using D ₂ O

Site-selective incorporation of deuterium into biologically active compounds is high interest in pharmaceutical industry. We present a mild and environmentally benign metal-free method for the remote selective radical C?H monodeuteration aliphatic bonds various amides with inexpensive heavy water (D2O) as source. The uses easily installed N-allylsulfonyl moiety an N-radical precursor that generates C-radical via site-selective 1,5- or 1,6-hydrogen atom transfer (HAT). Methyl thioglycolate, readily exchanges its proton D2O, serves deuteration reagent chain-carrier. highly has been applied to different types unactivated sp3-C?H also next heteroatoms. potential utility this further demonstrated by natural product derivatives drugs.