反应详情

9.8 g (32 mmol) of 7-chloro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxamidoxime were stirred in 60 ml of N,N-dimethylformamide with 7 g (41 mmol) of chloroacetic anhydride at room temperature for 1 hour and at 105° for 4 hours. After evaporating the solvent the residue was dissolved in methylene chloride and the solution was washed with saturated sodium bicarbonate solution and dried over magnesium sulfate. By evaporation of the solvent and chromatography of the residue on silica gel while eluting with ethyl acetate there were obtained 6.63 g (65%) of 7-chloro-3-(5-chloromethyl-1,2,4-oxadiazol-3-yl)-5-methyl-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-6-one.

1. customAfter evaporating the solvent the residue
2. dissolutionwas dissolved in methylene chloride
3. washthe solution was washed with saturated sodium bicarbonate solution
4. dry with materialdried over magnesium sulfate
5. customBy evaporation of the solvent and chromatography of the residue on silica gel
6. washwhile eluting with ethyl acetate