Tandem allylic substitution, WingPhos, Protecting-group-free, Palladium catalysis, Enantioselectivity, Chemical technology, TP1-1185, Biochemistry, QD415-436

A protecting-group-free enantioselective tandem allylic substitution of o-phenylenediamines and o-aminophenols is realized for the first time with a Pd-WingPhos catalyst, providing expedient access to a series of chiral vinyl-substituted heterocycles in excellent ee and yields under mild reaction conditions. The protocol is applied successfully to the synthesis of a cholesteryl ester transfer protein (CETP) inhibitor.