Palladium-Catalyzed Weak Chelation-Assisted Site-Selective C-H Arylation of N-Aryl Pyridones via 2-fold C-H Activation.

Palladium-catalyzed weak chelation-assisted oxidative cross-dehydrogenative coupling of arenes has been accomplished. The use of medicinally important pyridones as the intrinsic directing group, regioselectivity, 2-fold C-H activation, and late-stage modification of bioactive compounds are the important practical features.

Biorelevant Weakly Coordinating Directing Group Assisted C-H Alkenylation with Cyclopropanols via Sequential C-H/C-C Activation.

A weakly coordinating biorelevant intrinsic directing group (DG) assisted site-selective C-H alkenylation via sequential C-H/C-C bond activation has been accomplished under Ru(II)-catalysis using readily accessible cyclopropyl alcohol as an alkenyl surrogate. Utilization of an intrinsic DG, exclusive regioselectivity, functional group diversity, late-stage natural product and drug mutations are the important practical features.