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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1979376Generated: October 30, 2026

HCID 21201610, compound → 1-(2-toluoylmethyl)-2-oxo-3-amino-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepine

https://huagongshe.com/reaction/1979376

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHCID 21201610HCID 21201610—
Solvent1,4-Dioxane hydrochlorideHCID 20443148—
Product1-(2-toluoylmethyl)-2-oxo-3-amino-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepineHCID 2120161767%

Reaction Conditions

Temperature50 °C

Reaction Steps

1-(2-Toluoylmethyl) -2-oxo-3-tert-butoxycarbonylamino-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepine (1.00 g) was suspended in 4N HCl-dioxane (10 ml), the suspension was stirred at 50° C. for one hour. The reaction mixture was concentrated under reduced pressure, the residue was dissolved in water, the solution was washed with diethyl ether, alkaline with saturated aqueous sodium bicarbonate, and extracted with methylene chloride. The organic layer was dried over anhydrous sodium sulfate, the solvent was evaporated under reduced pressure, the residue was purified by silica gel column chromatography (ethyl acetate), to thereby obtain 538 mg of the titled compound.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06239131B1
Source datasetuspto-grants-2001_05
ORD IDord-67ec49765d614ae3b7e4cc33ff7ef4ac
Source noteuspto-grants-2001_05