SR49059的合成研究

Study on Synthesis of SR49059

以邻氯苯甲酸 ,3,4 二甲氧基苯磺酰氯 ,L 脯氨酸酰胺等为原料 ,通过醛醇缩合、傅克酰化和环合反应 ,合成了 2 (2S) 2 氨基甲酰吡咯烷基羰基 5 氯 3 (2 氯苯基 ) 1 (3,4 二甲氧基苯磺酰氯 ) 3 羟基 二氢吲哚 ,此法原料易得 ,操作简便 ,收率较高 .

chlorobenzic acid, 3,4-dimethoxybenzensulphonyl chloride and L-prolinamide undergo series reactions, such as Friedel-crafts acylation, Aldol reaction and cyclization, to get 2-((2S)-2- carbamoylpyrrolidinocarbony)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxyphenylsulfonyl)-3-hydroxyindoline, and the yield is high. The raw materials are easily obtainable and the operation is simple.