反应详情

A solution of 4-[6-(4-fluorobenzenesulfonyloxy)benzothiazol-2-ylcarbamoyl]-piperidine-1-carboxylic acid tert-butyl ester (intermediate 3) (100 mg, 0.187 mmol) and of TFA (0.5 ml) in dichloromethane (4.5 ml) is stirred at room temperature for 1 hour. The reaction medium is evaporated to dryness. The residue is taken up in a minimum amount of water, neutralized by addition of aqueous 10% Na2CO3 solution and extracted with ethyl acetate to give 55 mg of 4-fluorobenzenesulfonic 2-[(piperidine-4-carbonyl)amino]benzo-thiazol-6-yl ester (white solid).

1. customThe reaction medium is evaporated to dryness
2. additionneutralized by addition of aqueous 10% Na2CO3 solution
3. extractionextracted with ethyl acetate