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目的优化盐酸昂丹司琼的合成工艺。方法以1,2,3,9-四氢-4H-咔唑-4-酮为起始原料,经甲基化得9-甲基-1,2,3,9-四氢-4H-咔唑-4-酮(3),3与二甲胺盐酸盐、多聚甲醛、2-甲基咪唑经过“一锅烩”反应得到中间体9-甲基-3-[(2-甲基-1H-咪唑-1-基)甲基]-1,2,3,9-四氢-4H-咔唑-4-酮(4),4经成盐反应得到目标产物盐酸昂丹司琼。结果与结论目标化合物的结构经1H-NM R、M S谱确证,总收率为57.2%,该合成工艺步骤简便,收率较高,易于工业化生产。
Objective To optimize the synthesis of ondansetron hydrochloride. Methods Starting from 1,2,3,9-tetrahydro-4H-carbazol-4-one, methylation gave 9-methyl-1,2,3,9-tetrahydro-4H-carb (3) was reacted with dimethylamine hydrochloride, paraformaldehyde and 2-methylimidazole to obtain the intermediate 9-methyl-3 - [(2- Methyl-1H-imidazol-1-yl) methyl] -1,2,3,9-tetrahydro-4H-carbazol-4-one (4), 4 to obtain the desired product Ondansetron hydrochloride Joan. Results and Conclusions The structure of the target compound was confirmed by 1H-NMR and MS spectra. The total yield was 57.2%. The synthesis procedure was simple, the yield was high, and it was easy to be industrially produced.