Preparation of 2-pyridone-containing tricyclic alkaloid derivatives as potential inhibitors of tumor cell proliferation by regioselective intramolecular N- and C-acylation of 2-pyridone

A novel and practical preparation of 2-pyridone-containing tricyclic alkaloid derivatives was developed. By regioselective intramolecular N- and C-acylation of 2-(4-aryl-2-pyridon-6-yl)benzoic acid, a pair of structural isomers 2-aryl pyrido2,1-a]isoindole-4,6-diones and 4-aryl 1-methyl-1H-indeno1,2-b]-pyridine-2,5-diones, as potential inhibitors of tumor cell proliferation, were prepared respectively.