An Improved Synthesis of Etizolam

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 .