1,2-Dichloroethane → HCID 86637010, compound

Participants

Reaction Steps

2-Chloro-5-fluoro-6-[(3-thienylmethyl)amino]-4(1H)-pyrimidinone hydrazone dihydrochloride (1.0828 g) and (2R)-3-cyclopentyl-2-{[formyl(tetrahydro-2H-pyran-2-yloxy)amino]methyl}propanoic acid diisopropyl amine salt form (1.63 g, 3.8 mmol) were dissolved in DMF (9 mL). NMM (2.1 mL, 19.1 mmol) was added, followed by HOAt (0.512 g, 3.76 mmol) and EDC (0.722 g, 3.77 mmol). After stirring overnight, the reaction mixture was purified by RP-HPLC to provide [(2R)-3-(2-{2-chloro-5-fluoro-6-[(3-thienylmethyl)amino]-4-pyrimidinyl}hydrazino)-2-(cyclopentylmethyl)-3-oxopropyl](tetrahydro-2H-pyran-2-yloxy)formamide as a reddish brown solid (0.7045 g). LCMS: (M+H−THP)+=471.1.

Provenance & Evidence