Benzenesulfonamide → 2,5-dimethyl-N-[(1S)-1-(4-{[(phenylsulfonyl)amino]carbonyl}phenyl)ethyl]-4-[4-(trifluoromethyl)benzyl]thiophene-3-carboxamide

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Reaction Steps

4-{(1S)-1-[({2,5-Dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]ethyl}benzoic acid from Example 12 (200 mg, 0.433 mmol) was treated with benzenesulfonamide (85.0 mg, 0.542 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (166 mg, 0.866 mmol) and 4-dimethylaminopyridine (66.0 mg, 0.542 mmol) under conditions similar to Example 18. The crude was purified by Combi Flash chromatography system (25% THF/CHCl3 for 5 min., then 50% for 5 min.) to afford the desired product as a white solid. MS (−APCI): m/z 599 (M−1)−.

Provenance & Evidence