The utilization of the transient directing strategy into the direct oxidative dehydrogenative arylation of aldehydes with arenes was reported for the first time. Featured by mild reaction conditions, good functional group compatibility, and great regioselectivity, the method should find broad applications in new medicine and material development and discovery processes.

The palladium-catalyzed intramolecular C-H/C-H coupling reaction of two simple arenes to generate 6H-benzo[c]chromenes has been reported for the first time. The approach features broad substrate scope and good tolerance of functional groups and uses molecular oxygen as the terminal oxidant. The high efficiency of the approach is verified by concise total synthesis of natural product cannabinol.

A palladium-catalyzed asymmetric allyl-allyl cross-coupling reaction to construct the chiral quaternary carbon center of crinane alkaloids has been developed. On the basis of an efficient approach, the enantioselective synthesis of (-)-crinane (1) is presented, and the first asymmetric total synthesis of (+)-4a-dehydroxycrinamabine (2) was achieved by subsequent oxidation, 1,4-conjugate addition, RCM reaction, reductive amination, and Pictet-Spengler reaction. The method provided an alternative strategy for the syntheses of crinane alkaloids and other Amaryllidaceae natural products.