反应详情

2-Chloro-5-fluoro-6-hydrazino-N-methyl-N-(1,3-thiazol-2-ylmethyl)-4-pyrimidinamine (assumed dihydrochloride) (0.9034 g, 2.509 mmol) and (2R)-3-cyclopentyl-2-{[formyl(tetrahydro-2H-pyran-2-yloxy)amino]methyl}propanoic acid (1.299 g, 3.01 mmol) were dissolved in DMF (13 mL). NMM (1.655 mL, 15.05 mmol) was added, followed by HOAt (0.4095 g, 3.01 mmol) and EDC (0.577 g, 3.01 mmol). After stirring overnight, the reaction mixture was purified by RP-HPLC to provide [(2R)-3-(2-{2-chloro-5-fluoro-6-[methyl(1,3-thiazol-2-ylmethyl)amino]-4-pyrimidinyl}hydrazino)-2-(cyclopentylmethyl)-3-oxopropyl](tetrahydro-2H-pyran-2-yloxy)formamide as a red sticky material. LCMS: (M+H)+=570.2.

1. customthe reaction mixture was purified by RP-HPLC