依替唑仑是一种在临床上应用较为广泛的镇静、催眠、抗抑郁药。以2-氨基-3-（2-氯苯甲酰）-5-乙基噻吩（Ⅰ）为原料，经氯乙酰化，再在乙醇中与乌洛托品环合，制得关键中间体（Ⅲ）。中间体（Ⅲ）经硫化、环合反应制得依替唑仑（Ⅴ），4步反应总收率为56．4％。改进后的反应具有合成路线短、条件温和、操作简便、收率高等优点。%Etizolam is a sedative , hypnotic and antidepressant drug widely used in clinics .In this study , the key intermediate (Ⅲ) was synthesized through acetylation and then cyclization in ethanol with uro-tropin from 2-amino-3-( 2 -chlorobenzoyl ) -5 -ethylthiophene (Ⅰ) as raw material .The target product etizolam (Ⅴ) was successfully obtained from Ⅲvia sulfuration and cyclization .The total yield of the four steps was 56.4%.The improved synthetic process has such advantages as short synthetic route , mild reaction condition , simple operation , high yield and so on .
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