Successive hydrolysis and transfer hydrogenation of 2-chloroquinolines to 3,4-dihydroquinolones

Abstract

3,4-Dihydroquinolones are fundamental motifs widely found in a variety of natural products and drug molecules. Conventional methods for their synthesis suffer from the disadvantages of harsh reaction conditions and inefficiency, as well as selectivity issues. Herein, we develop a practical and efficient platform for the synthesis of 3,4-dihydroquinolones through successive hydrolysis and transfer hydrogenation processes. A wide range of 2-chloroquinolines and other substrates were compatible with this catalytic system and were converted into the corresponding products in moderate to excellent yields. The scale-up experiment and late-stage functionalization performance verified the practical use of this protocol.