| 盐酸阿扎司琼的合成 |
| |
| 引用本文： | 袁哲东,俞雄,王强,张秀平.盐酸阿扎司琼的合成[J].中国医药工业杂志,2006,37(1):1-3. |
| |
| 作者姓名： | 袁哲东 俞雄 王强 张秀平 |
| |
| 作者单位： | 上海医药工业研究院,上海,200437 |
| |
| 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-苯并嗯嗪-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％。
|
| 关 键 词： | 阿扎司琼 止吐药 合成 |
| 文章编号： | 1001-8255（2006）01-0001-03 |
| 收稿时间： | 2005 |
Synthesis of Azasetron Hydrochloride |
| |
| Authors: | YUAN Zhe-Dong YU Xiong WANG Qiang ZHANG Xiu-Ping |
| |
| Institution: | Shanghai Institute of Pharmaceutical Industry, Shanghai 200437 |
| |
| Abstract: | Azasetron hydrochloride was synthesized from methyl salicylate by chlorination, nitration, reduction to give methyl 3-amino-5-chloro-2-hydroxybenzoate, which subjected to cyclization with chloroacetyl chloride, methylation and hydrolysis to afford 6-chloro-4-methyl-3,4-dihydro-3-oxo-2H-1,4-benzoxazine-8-carboxylic acid, follow by chlorination, reaction with 3-aminoquinuclidine and then HCl salt formation with an overall yied of 37 %. |
| |
| Keywords: | azasetron antiemetic synthesis |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
|
