反应详情

A solution of tert-butyl (1S,2R)-2-(4-(1-(difluoromethyl)-1H-pyrazol-4-yl)-2-(2,4-dimethoxybenzyl)-7-fluoro-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)cyclohexylcarbamate (36 mg, 0.057 mmol) in TFA (2 mL) was heated at 60° C. for 2 h. After removal of the solvent, the residue was diluted in MeOH (2 mL) and was purified by preparative HPLC. The fractions were collected and stripped to dryness via rotary evaporation to yield the title compound as a TFA salt (18.7 mg, 86%). 1H NMR (500 MHz, DMSO-d6) δ ppm 1.40-1.52 (m, 2 H), 1.58-1.76 (m, 3 H), 1.75-1.94 (m, 3 H), 3.67 (br s, 1 H), 4.44 (d, J=4.88 Hz, 2 H), 4.53 (br s, 1 H), 6.86 (d, J=6.83 Hz, 1 H), 7.71 (br s, 2 H), 7.79-8.12 (m, 1 H), 8.53 (s, 2 H), 9.41 (s, 1 H). [M+H] calc'd for C17H19F3N6O, 381; found, 381.

1. customAfter removal of the solvent
2. additionthe residue was diluted in MeOH (2 mL)
3. customwas purified by preparative HPLC
4. customThe fractions were collected
5. customstripped to dryness via rotary evaporation