反应详情

1-[1-(2-Toluoylmethyl)-2-oxo-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-3-yl]-3-(3-methoxycarbonyl-4-chlorophenyl)urea (691 mg) was dissolved in methanol (30 ml), aqueous lithium hydroxide monohydrate (234 mg) solution (15 ml) and tetrahydrofuran (15 ml) were added, the mixture was refluxed for one hour. The reaction mixture was concentrated under reduced pressure, 1N hydrochloric acid was added, and extracted with methylene chloride. The organic layer was dried over anhydrous magnesium sulfate, the solvent was evaporated under reduced pressure, and diisopropyl ether was added to the residue for trituration, collected by filtration, to thereby obtain 437 mg of the titled compound.

1. temperaturethe mixture was refluxed for one hour
2. concentrationThe reaction mixture was concentrated under reduced pressure, 1N hydrochloric acid
3. additionwas added
4. extractionextracted with methylene chloride
5. dry with materialThe organic layer was dried over anhydrous magnesium sulfate
6. customthe solvent was evaporated under reduced pressure, and diisopropyl ether
7. additionwas added to the residue for trituration
8. filtrationcollected by filtration