【摘要】 水杨酸甲酯经氯化、硝化、还原制得3-氨基-5-氯-2-羟基苯甲酸甲酯,与氯乙酰氯环合、甲基化、水解制得6-氯-4-甲基-3,4-二氢-3-氧代-2H-1,4-苯并噁嗪-8-甲酸,再经氯化、与3-氨基奎宁环反应和成盐制得盐酸阿扎司琼,总收率37%。更多还原

【Abstract】 Azasetron hydrochloride was synthesized from methyl salicylate by chlorination, nitration, reduction togive methyl 3-amino-5-chloro-2-hydroxybenzoate, which subjected to cyclization with chloroacetyl chloride, methylation andhydrolysis to afford 6-chloro-4-methyl-3,4-dihydro-3-oxo-2H-1,4-benzoxazine-8-carboxylic acid, follow by chlorination, reac-tion with 3-aminoquinuclidine and then HCl salt formation with an overall yied of 37%.更多还原