摘要
目的 :改进盐酸阿洛司琼的合成工艺 ,以利于工业生产。方法 :以 2 ,4 -哌啶二酮 - 3-羧酸甲酯与 N -甲基苯肼缩合后在硫酸和醋酸存在下环合得制 2 ,3,4 ,5 -四氢 - 5 -甲基 - 1H-吡啶并 [4、3- b]吲哚 - 1-酮 ,然后甲基化 ,再与 4 -羟甲基 - 5 -甲基咪唑在对甲苯磺酸催化下缩合。结果 :制得合格的盐酸阿洛司琼 ,总收率 38%。结论 :经改进的工艺操作简便 。
AIMS to improve the preparation process of alosetron hydrochloride on a large scale production; METHODS Alosetron Hydrochloride was preparated by condensation methyl 2,4 piperidindione 3 carboxylate and N methyl phenyl hydrazine, then cyclization in sulfuric acid acetic acid,and condensation with 4 hydroxyl 5 methyimidazole. RESULTS the total yield is 38%. CONCLUSIONS the improved process is more convenient on a large scale production.
出处
《江苏药学与临床研究》
2002年第4期14-15,共2页
Jiangsu Pharmacertical and Clinical Research
