Hydroxylamine HCl → HCID 178513598, compound

Participants

Reaction Conditions

Reaction Steps

Trans-5-cyano-3-[4-(2-oxopyrrolidin-1-yl)cyclohexylcarbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (107 mg) obtained in Example 6 is suspended in dimethyl sulfoxide (2 ml), and thereto are added hydroxy-ammonium chloride (36 mg) and a 28% sodium methoxide in methanol (100 μl). The mixture is heated at 50° C. for 2 hours, and further at 80° C. for 2 hours. The reaction solution is poured into ice-water, and the precipitates are collected by filtration, and purified by recycle HPLC to give the title compound (25 mg; APCI-MS M/Z: 539/541 [M+H]+) and trans-5-aminocarbonyl-3-[4-(2-oxopyrrolidin-1-yl)cyclohexylcarbonylamino]-N-(5-chloropyridin-2-yl)benzofuran-2-carboxamide (18 mg; APCI-MS M/Z: 524/526 [M+H]+).

Provenance & Evidence