反应详情

5-Fluoro-4-hydrazino-2-methyl-6-(1-pyrrolidinyl)pyrimidine (69 mg, 0.33 mmol), (2R)-3-cyclopentyl-2-({formyl[(phenylmethyl)oxy]amino}methyl)propanoic acid (110 mg, 0.36 mmol), and HOAt (49 mg, 0.36 mmol) were dissolved in 2 mL of DMF. NMM (0.18 mL, 1.65 mmol) was added, followed by EDC (69 mg, 0.36 mmol). After stirring overnight at room temperature, the reaction mixture was purified by RP-HPLC to provide ((2R)-2-(cyclopentylmethyl)-3-{2-[5-fluoro-2-methyl-6-(1-pyrrolidinyl)-4-pyrimidinyl]hydrazino}-3-oxopropyl)[(phenylmethyl)oxy]formamide (90 mg, 55%).

1. customthe reaction mixture was purified by RP-HPLC