Diisopropylethylamine → HCID 56932773, compound

Participants

Reaction Steps

To a solution of 1,1,1-trifluoro-2-(4-((2S)-2-(((1-methylethyl)amino)methyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-2-propanol (0.100 g, 0.203 mmol, Example 195, Step 1) in CH2Cl2 (5.0 mL) was added 4-dimethylaminopyridine (0.005 g, 0.061 mmol), pyridine-3-sulfonyl chloride (0.072 g, 0.407 mmol, WAKO, Richmond, Va.) and Hünig's base (0.106 mL, 0.610 mmol). After 2 h at room temperature, the solvent was removed and the crude product was purified by column chromatography (40 g of silica, 20 to 40% acetone in hexanes) to give N-(1-methylethyl)-N-(((2R)-4-(2-thiophenylsulfonyl)-1-(4-(2,2,2-trifluoro-1-hydroxy-1-methylethyl)phenyl)-2-piperazinyl)methyl)-3-pyridinesulfonamide (0.120 g) as a mixture of two isomers.

Provenance & Evidence