Direct and Enantioselective Acylation of Diverse C(sp 3 )–H Bonds with Aldehydes

Chiral ketones containing α-aryl, α-amino, or α-oxy stereocenters are unique structural motifs found in numerous important natural products and pharmaceuticals, but their enantioselective synthesis remains a challenge. We report a synthetic method for the enantioselective acylation of diverse C(sp3)–H bonds by combining peroxide photosensitization and nickel catalysis. This method utilizes abundant and readily available aldehydes as an acyl source and is capable of acylating a variety of C(sp3)–H bonds, including benzylic, α-amino, and α-alkoxy C(sp3)–H bonds, with excellent enantioselectivity and atom economy. The practicability of this strategy is demonstrated in the enantioselective synthesis of chiral…

• NN
  National Natural Science Foundation of China

  Awards: 22301225, 22471203
• CP
  China Postdoctoral Science Foundation

  Award: 2024M752461
• BR
  Basic Research Program of Jiangsu Province

  Award: BK20250455
• BA
  Basic and Applied Basic Research Foundation of Guangdong Province

  Award: 2023A1515110137