反应详情

1.28 g (4.1 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, 25 ml of N,N-dimethylformamide, 2 ml (11.7 mmol) of N-ethyldiisopropylamine and 1.19 g (4.5 mmol) of α,α'-dibromo-o-xylene were stirred at room temperature for 4 hours. After evaporating the solvent the residue was chromatographed on 180 g of silica gel while eluting with ethyl acetate. The uniform fractions were evaporated. There was obtained 0.39 g (23%) of 5,6-dihydro-3-(3-isoindolin-2-ylmethyl-1,2,4-oxadiazol-5-yl)-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one, which was converted into the hydrochloride of m.p. 155°-160°.

1. customAfter evaporating the solvent the residue
2. customwas chromatographed on 180 g of silica gel
3. washwhile eluting with ethyl acetate
4. customThe uniform fractions were evaporated