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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1281027Generated: October 27, 2026

Ethyl Acetate → 1-(3-amino-4-chlorobenzyl)-4-[[N-(2-(tert-butoxycarbonylamino)-4,5-difluorobenzoyl)glycyl]aminomethyl]piperidine

https://huagongshe.com/reaction/1281027

Reaction equation

Participants

RoleNameHCIDCharge
ReactantEthyl AcetateHCID 8857—
Reactant4-[[N-(2-(tert-butoxycarbonylamino)-4,5-difluorobenzoyl)glycyl]aminomethyl]-1-(4-chloro-3-nitrobenzyl)piperidineHCID 18426159—
CatalystPalladiumHCID 23938—
SolventMethanolHCID 887—
Product1-(3-amino-4-chlorobenzyl)-4-[[N-(2-(tert-butoxycarbonylamino)-4,5-difluorobenzoyl)glycyl]aminomethyl]piperidineHCID 1842627768.9%

Reaction Steps

A mixture of 4-[{N-(2-(tert-butoxycarbonylamino)-4,5-difluorobenzoyl)glycyl}aminomethyl]-1-(4-chloro-3-nitrobenzyl)piperidine (121 mg, 0.20 mmol), 10% palladium-activated carbon (85 mg), ethyl acetate (10 mL), and methanol (1 mL) was stirred under a hydrogen atmosphere at room temperature for 19 h. The Pd catalyst was filtered off and the filtrate was concentrated to afford 1-(3-amino-4-chlorobenzyl)-4-[{N-(2-(tert-butoxycarbonylamino)-4,5-difluorobenzoyl)glycyl}aminomethyl]piperidine (78 mg, 68%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06451842B1
Source datasetuspto-grants-2002_09
ORD IDord-57440b74d1704aa98fd518a5c87b37cf
Source noteuspto-grants-2002_09