(2,5-difluorophenyl)methanesulfonyl chloride

Conditions: temp:0.00; pressure:0.00; stir:

Conditions: temp:0.00; pressure:0.00; stir:

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: At room temperature, (2,5-difluorophenyl)methanesulphonyl chloride (226 mg) is added to a solution of 4-{4-[(cyclohexyloxy)carbonyl]-1,3-thiazol-2-yl}piperidinium chloride (VII-1, 330 mg) and triethylamine (303 mg) in dichloromethane (5 ml). The mixture is stirred at room temperature overnight, and water is then added. The aqueous phase is separated off and extracted with ethyl acetate, and the combined organic phases are then dried with sodium sulphate. The solid is filtered off and the solvent is removed by distillation. The residue is purified chromatographically. This gives cyclohexyl 2-{1-[(2,5-difluorobenzyl)sulphonyl]piperidin-4-yl}-1,3-thiazole-4-carboxylate (156 mg, 32%). The aqueous phase is separated off extracted with ethyl acetate the combined organic phases are then dried with sodium sulphate The solid is filtered off the solvent is removed by distillation The residue is purified chromatographically