The invention relates to a synthesis method of 2-amino-5-chloro-N, 3-dimethyl
benzamide, which comprises the following steps:
hydrogenation reaction: adding 3-methyl-2-
nitrobenzoic acid,
palladium on carbon,
methanol,
nitrogen and
hydrogen for replacement; filtering to remove
palladium and carbon, adding
activated carbon into filtrate for decoloration, concentrating under reduced pressure, crystallizing, filtering and
drying; cyclization reaction: adding 3-methyl-2-
nitrobenzoic acid,
dichloromethane,
oxalyl chloride and
aluminum trichloride, reacting, separating liquid, removing a water phase, concentrating an organic phase under reduced pressure, cooling, crystallizing, filtering and
drying to obtain 2-amino-5-chloro-N, 3-dimethylbenzamide; 2-amino-5-chloro-N, 3-dimethylbenzamide,
ethanol, a catalyst PIDA and CuCl2 are sequentially added,
nitrogen displacement and stirring heating are carried out, a reaction is carried out for 12 h, a 10%
sodium bicarbonate aqueous solution is dropwise added until the pH value is 6.0-6.5, the temperature is reduced to the
room temperature, and filtering and
drying are carried out; and ring-opening reaction: adding 6-chloro-3-methyl itaconic anhydride and
purified water, replacing with
nitrogen, cooling, adding 40%
methylamine aqueous solution, heating, sampling, detecting reaction, cooling, crystallizing, filtering and drying.