反应详情

1.88 g (5 mmol) of (S)-8-chloro-1-(5-chloromethyl-1,2,4-oxadiazol-3-yl)-12,12a-dihydro-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepin-9-one were stirred at room temperature for 4 hours with 2 g (2.2 mmol) of bis(2-methoxyethyl)-amine and 15 ml of N,N-dimethylformamide. After evaporating the solvent the reaction mixture was taken up in 4N sodium hydroxide solution, whereupon the mixture was extracted three times with methylene chloride. By drying the organic phase over magnesium sulfate and evaporating the solvent there were obtained 2.2 g (93%) of (S)-8-chloro-1-[5-di(2-methoxyethyl)aminomethyl-1,2,4-oxadiazol-3-yl]-12,12a-dihydro-9H,11H-azeto[2,1-c]imidazo[1,5-a][1,4]benzodiazepin-9-one, which was converted into the hydrochloride of m.p. 188°-190°.

1. customAfter evaporating the solvent the reaction mixture
2. extractionwas extracted three times with methylene chloride
3. dry with materialBy drying the organic phase over magnesium sulfate
4. customevaporating the solvent there