反应详情

1-[1-(2-toluoylmethyl)-2-oxo-5-(3,3-dimethylbutanoyl)-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-3-yl]-3-(3-ethoxycarbonylphenyl)urea (442 mg) was dissolved in methanol (20 ml), aqueous lithium hydroxide monohydrate (151 mg) solution (10 ml) and tetrahydrofuran (10 ml) were added, and the mixture was refluxed for one hour. The reaction mixture was concentrated under reduced pressure, 1N hydrochloric acid was added to the residue, extracted with methylene chloride. The solvent was evaporated under reduced pressure, diisopropyl ether was added to the residue for trituration, collected by filtration, to thereby obtain 324 mg of the titled compound as colorless powder (Yield: 77.1%).

1. temperaturethe mixture was refluxed for one hour
2. concentrationThe reaction mixture was concentrated under reduced pressure, 1N hydrochloric acid
3. additionwas added to the residue
4. extractionextracted with methylene chloride
5. customThe solvent was evaporated under reduced pressure, diisopropyl ether
6. additionwas added to the residue for trituration
7. filtrationcollected by filtration