Chloroform → HCID 178507373, compound

Participants

Reaction Steps

Trans-5-nitro-3-[4-(2-oxopyrrolidin-1-yl)cyclohexylcarbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (2.50 g) obtained in Example 404 is suspended in ethanol/tetrahydrofuran (1:1, 400 ml), and thereto is added Raney nickel, and the mixture is stirred at room temperature under atmospheric hydrogen pressure for 12 hours. To the resulting yellow suspension is poured chloroform (200 ml), and the mixture is stirred at room temperature for 0.5 hour. The insoluble materials are removed by filtration, and the filtrate is concentrated under reduced pressure. The residue is purified by silica gel column chromatography (eluent: chloroform to chloroform/methanol=4/1), suspended in ethyl acetate/diethyl ether. The precipitates are collected by filtration, washed with diethyl ether, and dried to give trans-5-amino-3-[4-(2-oxopyrrolidin-1-yl)cyclohexylcarbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (1.94 g). This product (150 mg) is suspended in methanol, and the mixture is treated with 4N hydrogen chloride in dioxane to give the title compound (158 mg).

Provenance & Evidence