1,2-Dichloroethane → HCID 86636986, compound

Participants

Reaction Steps

To a stirred solution of (2R)-3-cyclopentyl-2-({formyl[(phenylmethyl)oxy]amino}methyl)propanoic acid (0.282 g, 0.92 mmol), 2-chloro-6-(cyclobutylamino)-5-fluoro-4(1H)-pyrimidinone hydrazone (0.225 g), HOAt (0.132 g, 0.97 mmol) and NMM (0.53 mL, 4.85 mmol) in DMF (5 mL) was added EDC (0.186 g, 0.97 mmol) and the reaction was stirred overnight. The mixture was diluted with ether, washed with water, and the aqueous layer was back extracted with ether. The organics were dried (Na2SO4) and concentrated in vacuo. The resulting residue was purified by RP-HPLC to provide [(2R)-3-{2-[2-chloro-6-(cyclobutylamino)-5-fluoro-4-pyrimidinyl]hydrazino}-2-(cyclopentylmethyl)-3-oxopropyl][(phenylmethyl)oxy]formamide as a brown oil (0.055 g). LCMS: (M+H)+=519.2.

Provenance & Evidence