Benzenesulfonyl chloride → N-(2-{1-[2-(5-methyl-3-trifluoromethyl-pyrazol-1-yl)-acetyl]-piperidin-4-yl}-thiazol-4-yl)-benzenesulfonamide

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-[4-(4-amino-thiazol-2-yl)-piperidin-1-yl]-2-(5-methyl-3-trifluoromethyl-pyrazol-1-yl)-ethanone (100 mg, 0.04 mmol) in dimethylacetamide (0.8 mL) is added diisopropylethylamine (8.6 μL, 0.28 mmol), followed by benzenesulfonyl chloride (8.8 mg, 0.05 mmol) at RT. After stirring 15 min at 60° C., the reaction mixture is purified directly by preparative HPLC to give N-(2-{1-[2-(5-methyl-3-trifluoromethyl-pyrazol-1-yl)-acetyl]-piperidin-4-yl}-thiazol-4-yl)-benzenesulfonamide (Compound No. I.g.025). MS: m/z=514 (M+1).

Provenance & Evidence