反应详情

To a solution of (S)-tert-butyl 2-(5-(N-allyl-N-(1,1,1-trifluoropropan-2-yl)sulfamoyl)pyridin-2-yl)-6-cyclopropyl-1H-indole-1-carboxylate (500 mg, 0.91 mmol) in acetonitrile was added pyrrolidine (0.35 mL, 4.55 mmol). The mixture was stirred at room temperature for 5 hrs and the solvent was evaporated. The residue was purified on silica gel eluting with 0 to 10% ethyl acetate in CH2Cl2 to provide (S)-N-allyl-6-(6-cyclopropyl-1H-indol-2-yl)-N-(1,1,1-trifluoropropan-2-yl)pyridine-3-sulfonamide (370 mg, 91% yield). MS m/z 450.2 M+H+; 1H NMR (500 MHz, CDCl3): δ 9.28 (1H, s), 8.85 (1H, s), 7.96 (1H, d, J=5.5 Hz), 7.74 (1H, d, J=9.5 Hz), 7.49 (1H, d, J=5.5 Hz), 7.09 (1H, s), 7.01 (1H, s), 6.82-6.80 (1H, m), 5.75 (1H, m), 5.16-5.10 (2H, m), 4.64-4.62 (1H, m), 3.89 (2H, d, J=5.0 Hz), 2.00-1.96 (1H, m), 1.35 (3H, d, J=6.0 Hz), 0.98-0.96 (2H, m), 0.75-0.72 (2H, m).

1. customthe solvent was evaporated
2. customThe residue was purified on silica gel eluting with 0 to 10% ethyl acetate in CH2Cl2