A New Dioxazolone for the Synthesis of 1,2‐Aminoalcohols via Iridium(III)‐Catalyzed C(sp ³ )−H Amidation

Vicinal aminoalcohols are widespread structural motifs in bioactive molecules. We report the development of a new dioxazolone reagent containing p-nitrophenyldifluoromethyl group, which 1. displays good safety profile; 2. shows remarkably high reactivity oxime-directed iridium(III)-catalyzed amidation unactivated C(sp3)−H bonds; 3. leads to amide products can be hydrolyzed under mild conditions. The reaction is mild, general and compatible with both primary C−H bonds tertiary secondary alcohols, as well cyclic alcohols. This method provides an easy access free 1,2-aminoalcohols after efficient cleavage oxime directing group activated amide.