Selective C–H acylation of quinolin-2(1H)-one with α-oxocarboxylic acids at the C3 position by sliver catalysis and its application in the synthesis of palbociclib

An efficient and selective method C3-H acylation of quinolin-2(1H)-one with at the C3 position has been developed. Active molecules containing acylquinolones were synthesized by silver-catalyzed decarboxylation of α-oxycarboxylic acids with quinolin-2(1H)-one in moderate to good yields. This reaction affords a broad substrate scope and good tolerance of functional groups. In addition, using this protocol, the marketed drug Palbociclib could be synthesized easily.