摘要
氟普唑仑是一种在临床上应用较为广泛的镇静、催眠、抗抑郁药,毒副作用小。以2-氨基-5-氯-2’-氟二苯甲酮(II)为起始原料,经氯乙酰化、环化,硫化、再与乙酰肼反应关环即可得到氟普唑仑(I)。改进后的合成路线步骤少,操作简单,条件温和,反应时间大大缩短,总产率可达53.5%,纯度可达99%以上。
Flualprazolam is a sedative,hypnotic and antidepressant drug widely used in clinics with little toxic and side effects.The target product flualprazolam(I)was obtained using 2-amino-5-chloro-2’-fluorobenzophenone(II)as the starting material,and then via chloroacetylation,cyclization,sulfidation,and then ring closure with acethydrazide.The improved synthetic route has the characteristics of short steps,easy operation,mild conditions,greatly shortened reaction time,total yield can reach 53.5%,and purity can reach more than 99%.
作者
李世伟
曾志伟
王鹏祥
洪恋
关金涛
LI Shi-wei;ZENG Zhi-wei;WANG Peng-xiang;HONG Lian;GUAN Jin-tao(School of Chemical and Environment Engineering,Wuhan Polytechnic University,Wuhan 430023,China)
出处
《武汉轻工大学学报》
2020年第2期35-38,共4页
Journal of Wuhan Polytechnic University
关键词
氟普唑仑
硫化
乙酰肼
改进
flualprazolam
sulfidation
acethydrazide
improvement
