节点文献
盐酸格拉司琼的合成
Synthesis of Granisetron Hydrochloride
【摘要】 以靛红为原料,经水解、重氮化、还原、环化、甲基化、酰氯化后与endo-9-甲基-9-氮杂双环[3.3.1]壬-3-胺反应得格拉司琼,再与盐酸成盐得盐酸格拉司琼,总收率32.8%。
【Abstract】 Granisetron hydrochloride was synthesized from isatin by hydrolysis,diazotization,reduction,cyclization, methylation and acyl chlorination to afford 1 methylindazole 3 carbonyl chloride,which was condensed with endo 9 methyl 9 azabicyclo[3.3.1]non 3 yl amine followed by salt formation to yield granisetron hydrochloride in overall yield of 32.8%.
【关键词】 盐酸格拉司琼;
5-HT3受体拮抗剂;
止吐药;
合成;
【Key words】 granisetron hydrochloride; 5 HT 3 antagonist; antiemetic; synthesis;
【Key words】 granisetron hydrochloride; 5 HT 3 antagonist; antiemetic; synthesis;
- 【文献出处】 中国医药工业杂志 ,CHINESE JOURNAL OF PHARMACEUTICALS , 编辑部邮箱 ,2000年02期
- 【分类号】R975.4
- 【被引频次】11
- 【下载频次】436