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    • 4. 发明授权
    • Method of preparing 10H-dibenzo[b,f][11,4]thiazepin-11-one
    • 制备10H-二苯并[b,f] [11,4]硫杂环庚烯-11-酮的方法
    • US07214793B2
    • 2007-05-08
    • US10533052
    • 2003-11-26
    • Byong-Sung KwakKi-Nam ChungKi-Ho KohHee-Jun Hwang
    • Byong-Sung KwakKi-Nam ChungKi-Ho KohHee-Jun Hwang
    • C07D281/16
    • C07D281/16
    • 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.
    • 公开了一种制备10H-二苯并[b,f] [1,4]硫杂吖庚因-11-酮的方法,包括在存在或不存在还原剂的情况下,将二硫代水杨酸与1-氯-2-硝基苯在碱性水溶液中反应 制备2-(2-硝基苯基硫基)苯甲酸; 在氢气,溶剂和非均相金属催化剂的存在下使2-(2-硝基苯基亚磺酰基)苯甲酸进行硝基还原,制备2-(2-氨基苯基硫基)苯甲酸; 并在酸催化剂存在或不存在下,在有机溶剂中直接环化2-(2-氨基苯基硫基)苯甲酸。 根据本发明的方法由于使用廉价的起始材料而是经济的,并且通过最小化有机溶剂的使用并且在没有羧酸活化的情况下进行直接环化,也是环境友好和有效的。
    • 10. 发明申请
    • Method of preparing 10th-dibenzo[b,f][11,4]thiazepin-11-one
    • 制备10-二苯并[b,f] [11,4]硫杂环丁烷-11-酮的方法
    • US20070066589A1
    • 2007-03-22
    • US10533052
    • 2003-11-26
    • Byong-Sung KwakKi-Nam ChungKi-Ho KohHee-Jun Hwang
    • Byong-Sung KwakKi-Nam ChungKi-Ho KohHee-Jun Hwang
    • A61K31/554
    • C07D281/16
    • 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.
    • 公开了一种制备10H-二苯并[b,f] [1,4]硫杂吖庚因-11-酮的方法,包括在存在或不存在还原剂的情况下,将二硫代水杨酸与1-氯-2-硝基苯在碱性水溶液中反应 制备2-(2-硝基苯基硫基)苯甲酸; 在氢气,溶剂和非均相金属催化剂的存在下使2-(2-硝基苯基亚磺酰基)苯甲酸进行硝基还原,制备2-(2-氨基苯基硫基)苯甲酸; 并在酸催化剂存在或不存在下,在有机溶剂中直接环化2-(2-氨基苯基硫基)苯甲酸。 根据本发明的方法由于使用廉价的起始材料而是经济的,并且通过最小化有机溶剂的使用并且在没有羧酸活化的情况下进行直接环化,也是环境友好和有效的。