Iridium-Catalyzed Enantioselective α‑C(sp³)–H Borylation of Azacycles

We herein report an iridium-catalyzed enantioselective α-C­(sp3)–H borylation of a wide range of azacycles. The combination of an iridium precursor and a chiral bidentate boryl ligand has been shown to effectively differentiate enantiotropic methylene C–H bonds from a single carbon center, affording a variety of synthetically useful azacycles from readily available starting materials with good to excellent enantioselectivities.本文报道了一种铱催化的对映选择性α-碳(sp³)-氢硼化反应，可适用于多种氮杂环化合物。该体系采用铱前驱体与手性双齿硼配体组合，能够有效区分单个碳中心上的对映异构亚甲基C-H键，以易得的起始原料为底物，制备得到多种具备合成应用价值的氮杂环产物，且反应的对映选择性优良至优异。