An Iridium/Aluminum Cooperative Strategy for the β-C(sp )-H Borylation of Saturated Cyclic Amines.

Despite the widespread success in the functionalization of C(sp )-H bonds, the deliberate functionalization of C(sp )-H bonds in a highly site- and stereoselective manner remains a longstanding challenge. Herein, we report an iridium/aluminum cooperative catalytic system that enables the β-selective C-H borylation of saturated cyclic amines and lactams. Furthermore, we have accomplished an enantioselective variant using binaphthol-derived chiral aluminum catalysts to forge C-B bonds with high levels of stereocontrol.

Phase-transfer-catalysed asymmetric synthesis of 2,2-disubstituted 1,4-benzoxazin-3-ones.

1,4-Benzoxazin-3-one is a scaffold which is found in a variety of biologically active molecules. Because of its unique structure and drug-like activities, 1,4-benzoxazin-3-ones have been widely used in drug discovery. However, just a few methods have been developed to access these molecules by catalytic asymmetric synthesis.

Indanol-Based Chiral Organoiodine Catalysts for Enantioselective Hydrative Dearomatization.

Rapid development in the last decade has rendered chiral organoiodine(I/III) catalysis a reliable methodology in asymmetric catalysis. However, due to the severely limited numbers of effective organoiodine catalysts, many reactions still give low to modest enantioselectivity. We report herein a solution to this issue through the introduction of a pivotal indanol scaffold to the catalyst design.