反应详情

To the solution of 2-(4-(6-fluoro-1-(phenylsulfonyl)-1H-indol-3-yl)-1H-pyrazol-1-yl)ethanamine hydrochloride (Intermediate 19; 228 mg; 0.54 mmol) and DMAP (3 mg; 0.02 mmol) in pyridine (4 mL), was added MsCl (0.07 mL; 0.90 mmol) under nitrogen at 0° C. The reaction was warmed to r.t. and stirred overnight. The reaction mixture was concentrated and the residue was diluted with EtOAc (20 mL), washed with aqueous HCl (10 mL; 1 M), water (10 mL), brine (10 mL). The organic layer was dried over anhydrous Na2SO4, filtered, and concentrated to afford 300 mg of the title compound as a yellow solid, which was used directly without further purification.

1. concentrationThe reaction mixture was concentrated
2. additionthe residue was diluted with EtOAc (20 mL)
3. washwashed with aqueous HCl (10 mL; 1 M), water (10 mL), brine (10 mL)
4. dry with materialThe organic layer was dried over anhydrous Na2SO4
5. filtrationfiltered
6. concentrationconcentrated