反应详情

2 g (6.44 mmol) of 3-(3-aminomethyl-1,2,4-oxadiazol-5-yl)-5,6-dihydro-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one, 20 ml of N,N-dimethylformamide, 3.8 ml (22.5 mmol) of N-ethyldiisopropylamine and 1.6 ml (14.8 mmol) of bromomethylcyclopropane were stirred at 80° for 4 hours. After evaporating the solvent the residue was dissolved in methylene chloride and the solution was washed with water, dried and concentrated. By chromatography on 220 g of silica gel while eluting with methylene chloride/ethyl acetate 1/1 there were obtained 1.3 g (48%) of 3-[3-(bis-cyclopropylmethylaminomethyl)-1,2,4-oxadiazol-5-yl ]-5,6-dihydro-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one, which was converted into the hydrochloride of m.p. 170°-174°.

1. customAfter evaporating the solvent the residue
2. dissolutionwas dissolved in methylene chloride
3. washthe solution was washed with water
4. customdried
5. concentrationconcentrated
6. washBy chromatography on 220 g of silica gel while eluting with methylene chloride/ethyl acetate 1/1 there