止吐药昂丹司琼的合成  

Synthesis of Ondansetron Hydrochloride

作　　者：芦金荣[1] 施欣忠[1] 

机构地区：[1]中国药科大学有机化学教研室,南京210009

出　　处：《中国药科大学学报》1999年第4期246-248,共3页Journal of China Pharmaceutical University

摘　　要：以１ ，３环己二酮为起始原料，形成单苯腙后，经过环合、甲基化得９甲基１ ，２ ，３ ，９四氢４ Ｈ咔唑４酮（３） ，与吗啉及多聚甲醛进行 Ｍａｎｎｉｃｈ 反应，再与２甲基咪唑反应、成盐得标题化合物，总收率为４９１ ％ 。An improved process for the preparation of ondansetron hydrochloride (1) is described . Compound 1 wassynthesized from 1 ,2 ,3 ,9 tetrahydro 9 methyl 4 H carbazol 4 one(3) by Mannich reaction and condensation with 2 methylimidazole . The compound 3 was prepared from 1 , 3 cyclohexanedione through formation ofmonophenylhydrazone ,cyclization and methylation . The overall yield was 49 .1 % . The physical constants and spectradata of the title compound and that of some intermediate have been reported .

关 键 词：昂丹司琼 MANNICH反应 合成 合成 止吐药 

分 类 号：TQ463.53[化学工程—制药化工] R975.4[医药卫生—药品]