Herein, we describe the preparation of 1-tetralones bearing a remote quaternary stereocenter in a highly enantioselective manner. A sequence of Pd-catalyzed asymmetric 1,4-addition and Rh-catalyzed enantiospecific C-C/C-H activation delivers diverse 1-tetralones with a C4 quaternary stereocenter, which are prepared in good overall yields and high enantioselectivity.
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