三组分一锅合成1,4-苯并硫氮杂卓衍生物

A One-pot Three-component Reaction Providing 1,4-benzoxazepine Derivatives

苯并硫氮杂卓衍生物是一类重要的七元杂环化合物,有着重要的药理活性和生物活性,它的某些衍生物已经作为催眠药物、抗焦虑药物和心血管药物应用于临床。本文用4-氯苯甲醛、2-氨基苯硫酚和季酮酸为原料,二氯乙烷为溶剂,多组分反应一步合成三环1,4-苯并硫氮杂卓衍生物,实验产率高,条件温和。目标化合物的结构经红外光谱、氢谱、碳谱和高分辨质谱进行了表征。

Benzothiazepine is a very important heterocycle for its biological activities,which has important pharmacological activities and biological activities.Some of its derivatives have been used as hypnotics,antianxiety drugs and cardiovascular drugs in clinical practice.A new one-pot,three-component reaction of 4-chlorobenzaldehyde,2-aminobenzenethiol and tetronic acid for the synthesis of tricyclic 1,4-benzothiazepine derivatives in moderate to good yields was described.The structure of the target compound was characterized by IR,H-NMR,C-NMR and HR-M.