反应详情

To a solution of (3R)-tert-butyl 3-(6-(5-(2,6-difluorophenyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-3-yl)pyrazin-2-ylamino)pyrrolidine-1-carboxylate (280 mg, 0.486 mmol) in DCM was added TFA (0.5 ml, 6.49 mmol). The reaction was stirred at RT for 2 h, and then TFA was removed. The residue was purified with RP-HPLC to give (R)-6-(5-(2,6-difluorophenyl)-1H-indazol-3-yl)-N-(pyrrolidin-3-yl)pyrazin-2-amine as an orange solid. MS (ESI, pos. ion) m/z: 393 (M+1); 1H NMR (400 MHz, DMSO-d6) δ ppm 8.71 (1 H, s), 8.47 (1 H, s), 7.87 (1 H, s), 7.72 (1 H, d, J=8.6 Hz), 7.41-7.55 (2 H, m), 7.18-7.31 (3 H, m), 4.22-4.36 (1 H, m), 2.88-3.05 (2 H, m), 2.61-2.82 (2 H, m), 1.97-2.12 (1 H, m), 1.57-1.73 (1 H, m).

1. customTFA was removed
2. customThe residue was purified with RP-HPLC