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.