Ethanol hydrochloride → 1-{[(6S,7R)-7-(4-chloro-3-fluorophenyl)-1,4-oxazepan-6-yl]methyl}pyridin-2(1H)-one monohydrochloride
Reaction equation
Cl.C(O)C.[Cl:5][C:6]1[CH:11]=[CH:10][C:9]([C@@H:12]2[O:18][CH2:17][CH2:16][N:15](C(OC(C)(C)C)=O)[CH2:14][C@H:13]2[CH2:26][N:27]2[CH:32]=[CH:31][CH:30]=[CH:29][C:28]2=[O:33])=[CH:8][C:7]=1[F:34]>C(O)C>[ClH:5].[Cl:5][C:6]1[CH:11]=[CH:10][C:9]([C@@H:12]2[O:18][CH2:17][CH2:16][NH:15][CH2:14][C@H:13]2[CH2:26][N:27]2[CH:32]=[CH:31][CH:30]=[CH:29][C:28]2=[O:33])=[CH:8][C:7]=1[F:34]Participants
4
Procedure
14 N Hydrogen chloride-ethanol solution (1 mL, 14.00 mmol) was added to a solution (3 mL) of tert-butyl (6R,7R)-7-(4-chloro-3-fluorophenyl)-6-[(2-oxopyridin-1(2H)-yl)methyl]-1,4-oxazepane-4-carboxylate (267 mg, 0.61 mmol) in ethanol, and the mixture was stirred at room temperature for 3 hr. The residue was concentrated, diethyl ether was added, and the mixture was stirred for a while. The insoluble material was collected by filtration to give the title compound (227 mg, 0.608 mmol, 100%).