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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1979360Generated: October 30, 2026

HCID 21201753, compound → 1-(thiophen-3-yl)carbonylmethyl-2-oxo-3-amino-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepine

https://huagongshe.com/reaction/1979360

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHCID 21201753HCID 21201753—
Solvent1,4-Dioxane hydrochlorideHCID 20443148—
Product1-(thiophen-3-yl)carbonylmethyl-2-oxo-3-amino-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepineHCID 21201699100%

Reaction Conditions

Temperature57.5 °C

Reaction Steps

1-(Thiophen-3-yl)carbonylmethyl-2-oxo-3-tert-butoxycarbonylamino-5-pivaloyl-8-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepine (0.94 g) was dissolved in 4N HCl-dioxane (10 ml), the solution was stirred for one hour at 55-60° C. The react ion mixture was concentrated under reduced pressure, the residue was neutralized with saturated aqueous sodium bicarbonate, and extracted with methylene chloride. The organic layer was successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and the solvent was evaporated under reduced pressure, to thereby obtain 0.69 g of the titled compound as a brown solid(Yield: 100%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06239131B1
Source datasetuspto-grants-2001_05
ORD IDord-421bc303a24a45818f0a363f8c758761
Source noteuspto-grants-2001_05