(R)-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)-N,4-dimethylpentanamide → (R)-2-(7-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)-N,4-dimethylpentanamide

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Reaction Steps

A solution of (R)-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)-N,4-dimethylpentanamide (38 mg, 0.072 mmol) in TFA (5 mL) was heated to 65° C. for 4 h. After removal of the solvent, the residue was diluted in MeOH (2 mL) and was purified by preparative HPLC eluting with water (0.05% TFA) and ACN (25-30%, gradient, 0.035% TFA). The collected fractions were stripped to dryness to give the title compound. 1H NMR (500 MHz, DMSO-d6) δ ppm 0.84-0.93 (m, 6 H), 1.63-1.81 (m, 2 H), 2.57 (d, J=4.39 Hz, 3 H), 3.88 (s, 3 H), 4.04-4.19 (m, 2 H), 4.36 (s, 2 H), 6.99 (d, J=7.32 Hz, 1 H), 7.61-7.76 (m, 1 H), 7.93 (d, J=4.39 Hz, 1 H), 8.30 (s, 1 H), 8.83 (s, 1 H). [M+H] calc'd for C18H23FN6O2, 375; found, 375.

Provenance & Evidence