1,2-Dichloroethane → HCID 86637021, compound

Participants

Reaction Steps

2-Chloro-5-fluoro-6-{[2-(3-thienyl)ethyl]amino}-4(1H)-pyrimidinone hydrazone as a brown sticky solid (0.1401 g) and (2R)-3-cyclopentyl-2-{[formyl(tetrahydro-2H-pyran-2-yloxy)amino]methyl}propanoic acid (0.253 g, 0.586 mmol) were dissolved in DMF (7 mL). NMM (0.27 mL, 2.90 mmol) was added, followed by HOAt (0.080 g, 0.588 mmol) and EDC (0.112 g, 0.584 mmol). After stirring overnight, the reaction mixture was purified by RP-HPLC to provide [(2R)-3-[2-(2-chloro-5-fluoro-6-{[2-(3-thienyl)ethyl]amino}-4-pyrimidinyl)hydrazino]-2-(cyclopentylmethyl)-3-oxopropyl](tetrahydro-2H-pyran-2-yloxy)formamide as an orange solid (0.1677 g). LCMS: (M+H)+=569.3.

Provenance & Evidence