反应详情

8-{[2-(tert-Butoxycarbonyl-isopropyl-amino)-ethyl]-cyclopropyl-sulfamoyl}-4-oxo-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-propyl carboxylate is prepared according to synthesis 111, from 326 mg (1 mmol) of 8-chlorosulfonyl-4-oxo-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-carboxylic acid and 288 mg (1.2 mmol) of N-tert-butoxycarbonyl-N′-cyclopropyl-N-isopropyl-ethane-1,2-diamine to give, after esterification according to general method C (using di-n-propylsulfate as the dialkylsulfate) and purification by chromatography on silica (eluent cyclohexane/ethyl acetate 1/1 then 1/3), 201 mg (35% in two stages) of 8-{[2-(tert-butoxycarbonyl-isopropyl-amino)-ethyl]-cyclopropyl-sulfamoyl}-4-oxo-4,5-dihydro-3H-pyrrolo[2,3-c]quinoline-1-propyl carboxylate in the form of a white solid.

1. customto give
2. custompurification by chromatography on silica (eluent cyclohexane/ethyl acetate 1/1