1-(4-FLUORO-BENZENESULFONYL)-PIPERIDIN-4-YLAMINE synthesis

Yield:-

Reaction Conditions:

with trifluoroacetic acid in dichloromethane at 20; for 1 h;

Steps:

11.F

To a solution of compound E of this example (250 mg) in dichloromethane (0.5 mL) was added TFA (0.5 mL) and stirred at RT. After 1 h, the volatiles were removed in vacuo and the residue was treated with aqueous 2N NaOH and extracted with dichloromethane. The organic layer was separated, dried and concentrated to afford l-(4-fluorophenylsulfonyl)piperidin-4-amine as a solid. LC/MS; (M+H)⁺ = 259 which was used without further purification.

References:

WO2008/60907,2008,A2 Location in patent:Page/Page column 41