Trifluoroacetic acid → 6-((1S,2R)-2-Aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridin-3(2H)-one

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl (1R,2S)-2-(2-(2,4-dimethoxybenzyl)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)cyclohexylcarbamate (41.5 mg, 0.070 mmol) and TFA (2 mL) was heated at 65° C. for 3 h. Following reaction, the solvent was removed in vacuo. The residue was diluted with DMSO and MeOH (1/1), passed through a microfiltration frit, and purified via preparative HPLC. The fractions were collected and dried in vacuo to give a TFA salt of the title compound as a white solid (22 mg, 92%). 1H NMR (500 MHz, CD3OD) δ ppm 1.56-2.01 (m, 8 H), 3.85 (br s, 1 H), 3.94 (br s, 3 H), 4.45 (br s, 2 H), 4.67 (br s, 1 H), 8.31 (br s, 1 H), 8.81 (br s, 1 H). [M+H] calc'd for C17H21FN6O, 345; found, 345.

Provenance & Evidence