反应详情

(2R)-3-Cyclopentyl-2-({formyl[(phenylmethyl)oxy]amino}methyl)propanoic acid (0.238 g, 0.78 mmol), 2-chloro-5-fluoro-6-{[2-methyl-2-(4-morpholinyl)propyl]amino}-4(1H)-pyrimidinone hydrazone (0.249 g), NMM (0.26 mL, 2.35 mmol), HOAt (0.106 g, 0.78 mmol), EDC (0.150 g, 0.78 mmol) and DMF (4 mL) were combined, and the solution was stirred overnight. Purification by RP-HPLC provided [(2R)-3-[2-(2-chloro-5-fluoro-6-{[2-methyl-2-(4-morpholinyl)propyl]amino}-4-pyrimidinyl)hydrazino]-2-(cyclopentylmethyl)-3-oxopropyl][(phenylmethyl)oxy]formamide as a brown oil (0.169 g). LCMS: (M+H)+=606.3.

1. customPurification by RP-HPLC