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%。
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%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2000年第2期49-50,共2页
Chinese Journal of Pharmaceuticals
关键词
盐酸格拉司琼
止吐药
合成
granisetron hydrochloride
5 HT 3 antagonist
antiemetic
synthesis
