Ethanol hydrochloride → 1-{[(6S,7R)-7-(4-chloro-3-fluorophenyl)-1,4-oxazepan-6-yl]methyl}-3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)pyridin-2(1H)-one monohydrochloride

Participants

Reaction Steps

14 N Hydrogen chloride-ethanol solution (0.5 ml, 7.00 mmol) was added to a solution of tert-butyl (6R,7R)-7-(4-chloro-3-fluorophenyl)-6-{[2-oxo-3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)pyridin-1(2H)-yl]methyl}-1,4-oxazepane-4-carboxylate (180 mg, 0.35 mmol) in ethanol (2 mL), and the mixture was stirred at room temperature for 3 hr. The reaction mixture was diluted with ethanol (4 ml), and the mixture was heated under reflux for 10 min. The precipitated crystals were collected by filtration to give the title compound (149 mg, 0.325 mmol, 94%).

Provenance & Evidence