反应详情

To a solution of [(2R)-2-(cyclopentylmethyl)-3-(2-{6-[4-(dimethylamino)-3,3-dimethyl-1-pyrrolidinyl]-5-fluoro-2-methyl-4-pyrimidinyl}hydrazino)-3-oxopropyl][(phenylmethyl)oxy]formamide (0.0775 g, 0.136 mmol) in MeOH (5 mL) was added 10% Pd/C (50% water, 23 mg). The mixture was hydrogenated under balloon pressure for 1 h, and then filtered. The solution was concentrated in vacuo, and the residue was crystallized from EtOAc-hexanes to afford [(2R)-2-(cyclopentylmethyl)-3-(2-{6-[4-(dimethylamino)-3,3-dimethyl-1-pyrrolidinyl]-5-fluoro-2-methyl-4-pyrimidinyl}hydrazino)-3-oxopropyl]hydroxyformamide (0.0566 g, 87% yield, mixture of diastereomers) as an off-white solid. LCMS: (M+H)+: 480.1.

1. filtrationfiltered
2. concentrationThe solution was concentrated in vacuo
3. customthe residue was crystallized from EtOAc-hexanes