Enantioselective Intramolecular Copper‐Catalyzed Borylacylation

An enantioselective copper‐catalyzed intramolecular borylacylation is reported. The reaction proceeds through an initial enantioselective borylcupration of the styrene, followed by a nucleophilic attack on the tethered carbamoyl chloride. The products, chiral borylated 3,3‐disubstituted oxindoles, were generated in excellent yields and enantioselectivities. The versatile carbon–boron bond provides a platform for a wide array of diversification. Cu again: Chiral 3,3‐disubstituted borylated oxindoles have been synthesized in good yields and enantioselectivities. The reaction employs a chiral copper catalyst for an enantioselective borylcupration followed by intramolecular acylation with a tethered carbamoyl chloride. The chiral oxindole products are readily diversifiable into a range of substituted oxindole products. pin=pinacol.