【摘要】 以 4 -氯 - 3-磺胺基苯甲酸 ,2 ,3-二氢 - 2 -甲基 - 1H-吲哚和硫酸羟胺为原料 ,经 4步反应合成了降压新药吲哒帕胺 . 4 -氯 - 3-磺胺基苯甲酸与亚硫酰氯反应得 4 -氯 - 3-磺胺基苯甲酰氯 ( ) ,产率 97.4 % ;硫酸羟胺与发烟硫酸反应得羟胺 - O-磺酸 ( ) ,产率 94 .7% ;2 ,3-二氢 - 2 -甲基 - 1H-吲哚与 ( )反应生成 1-氨基 - 2 ,3-二氢 - 2 -甲基 - 1H-吲哚的盐酸盐 ( ) ,产率 81.7% ;( )和 ( )反应得目标产物吲哒帕胺 ( ) ,产率 77.4 % .并给出了 ( )和( )的提纯方法 .更多还原

【Abstract】 Indapamide(Ⅳ) was prepared by four step reactions, starting from 4 chloro 3 sulphamoyl benzoic acid, 1 amino 2,3 dihydro 2 methyl 1 H indole and hydroxylamine O sulphonic acid. 4 chloro 3 sulphamoyl benzoyl chloride(Ⅰ) was prepared by the reaction of 4 chloro 3 sulphamoyl benzoic acid and thionyl chloride, yield 97 4%. Hydroxylamine O sulphonic acid(Ⅱ) was prepared by the reaction of hydroxylamine with 25% oleum, yield 94 7%. 1 amino 2,3 dihydro 2 methyl 1 H indole hydrochloride(Ⅲ) was obtained by the reaction of 2,3 dihydro 2 methyl 1 H indole with Ⅱ, yield 81 7%. Ⅲ was reacted with Ⅰ to give the title compound Ⅳ, yield 77 4%. Methods of purification of Ⅲ and Ⅳ were also described.更多还原