Disclosed is a method of preparing 10H-dibenzo[b,f][1,4]thiazepin-11-one, including reacting dithiosalicylic acid with 1-chloro-2-nitrobenzene in a basic aqueous solution in the presence or absence of a reducing agent, to prepare 2-(2-nitrophenylsulfuryl)benzoic acid; subjecting the 2-(2-nitrophenylsulfuryl)benzoic acid to nitro group reduction in the presence of hydrogen, a solvent and a heterogeneous metal catalyst, to prepare 2-(2-aminophenylsulfuryl)benzoic acid; and directly cyclizing the 2-(2-aminophenylsulfuryl)benzoic acid in an organic solvent in the presence or absence of an acid catalyst. The method according to the present invention is economical due to the use of the inexpensive starting material, and also environmentally friendly and efficient by minimizing the use of the organic solvent and performing direct cyclization without the activation of carboxylic acid.
本发明公开了一种制备10H-二苯并[b,f][1,4]
噻吩-11-酮的方法,包括在碱性
水溶液中存在或不存在还原剂的情况下,将二
硫基
水杨酸与1-
氯-2-
硝基苯反应,制备2-(2-
硝基苯基磺酰基)
苯甲酸;在
氢气、溶剂和异相
金属催化剂的存在下,对2-(2-
硝基苯基磺酰基)
苯甲酸进行硝基还原,制备2-(2-
氨基苯基磺酰基)
苯甲酸;并在有机溶剂存在或不存在酸性催化剂的情况下,直接环化2-(2-
氨基苯基磺酰基)
苯甲酸。本发明的方法由于使用了廉价的起始材料,因此经济实惠,并且通过最小化有机溶剂的使用和在不激活
羧酸的情况下进行直接环化,具有环保和高效的特点。