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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1979366Generated: October 28, 2026

1,4-Dioxane hydrochloride → 1-tert-butylcarbonylmethyl-2-oxo-3-amino-5-phenyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepine

https://huagongshe.com/reaction/1979366

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1,4-Dioxane hydrochlorideHCID 20443148—
Reactant1-tert-butylcarbonylmethyl-2-oxo-3-tert-butoxycarbonylamino-5-phenyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepineHCID 21202016—
SolventEthanolHCID 702—
Product1-tert-butylcarbonylmethyl-2-oxo-3-amino-5-phenyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepineHCID 21201941100%

Reaction Conditions

Temperature50 °C

Reaction Steps

4N HCl-dioxane (5 ml) was added to a solution of 1-tert-butylcarbonylmethyl-2-oxo-3-tert-butoxycarbonylamino-5-phenyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepine (100 mg) in ethanol (5 ml ), the mixture was stirred at 50° C. for 30 minutes. The reaction mixture was concentrated under reduced pressure, the residue was neutralized with saturated aqueous sodium bicarbonate, extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate, the solvent was evaporated under reduced pressure, to thereby obtain 78 mg of the titled compound (Yield: 100%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06239131B1
Source datasetuspto-grants-2001_05
ORD IDord-4830f9c7d68f47ed9007544e5149c8e4
Source noteuspto-grants-2001_05