The invention discloses a quinolinone derivative and a preparation method thereof, and the quinolinone derivative comprises a 3-phenyl-6, 7-dimethoxy isoquinolin-1 (2H)-one derivative and a 3-phenyl-6, 7-dimethoxy quinolin-2 (1H)-one derivative which are shown in the structural general formulas of formula (I) and formula (II). Wherein 4, 5-dimethoxy-2-methyl
benzaldehyde is synthesized firstly, then the 4, 5-dimethoxy-2-methyl
benzaldehyde and substituted cyanophenyl are subjected to
cycloaddition reaction under the action of
potassium tert-butoxide and LiHMDS, and the 4, 5-dimethoxy-2-methyl
benzaldehyde is obtained; the preparation method of the 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl)
acetamide comprises the following steps: synthesizing 2-amino-4, 5-dimethoxybenzaldehyde, carrying out
acylation reaction on the 2-amino-4, 5-dimethoxybenzaldehyde and substituted
phenylacetic acid under the action of
HATU to obtain 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl)
acetamide, and carrying out cyclization reaction on the 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl)
acetamide under the action of K2CO3 to obtain the 2-(substituted phenyl)-N-(2-formyl-4, 5-dimethoxyphenyl) acetamide. The preparation method has the characteristics of mild
reaction conditions, simplicity in operation, high efficiency, environment friendliness and the like.