Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 490577Generated: October 30, 2026

1-Hydroxybenzotriazole → 2-[4-(2-Cyano-phenyl)-piperazine-1-carbonyl]-4-[(benzyl)-(2,2,2-trichloroethoxycarbonyl)-amino]-pyrrolidine-1-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/490577

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1-HydroxybenzotriazoleHCID 75771—
Reactant1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
ReactantN-(2-Cyanophenyl)piperazineHCID 2735875—
Reactant4-[(Benzyl)-(2,2,2-trichloro-ethoxycarbonyl)-amino]-pyrrolidine-1,2-dicarboxylicacid 1-tert-butyl esterHCID 67547735—
SolventDichloromethaneHCID 6344—
SolventTriethylamineHCID 8471—
Product2-[4-(2-Cyano-phenyl)-piperazine-1-carbonyl]-4-[(benzyl)-(2,2,2-trichloroethoxycarbonyl)-amino]-pyrrolidine-1-carboxylic acid tert-butyl esterHCID 67546549—

Reaction Steps

To a solution of 4-[(benzyl)-(2,2,2-trichloro-ethoxycarbonyl)-amino]-pyrrolidine-1,2-dicarboxylicacid 1-tert-butyl ester, HOBt, 1-(2-cyanophenyl)piperazine in DCM are added Et3N and EDC.HCl. The mixture is stirred overnight, then washed with citric acid, Na2CO3, brine, dried and concentrated to give 2-[4-(2-cyano-phenyl)-piperazine-1-carbonyl]-4-[(benzyl)-(2,2,2-trichloroethoxycarbonyl)-amino]-pyrrolidine-1-carboxylic acid tert-butyl ester (21)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07528136B2
Source datasetuspto-grants-2009_05
ORD IDord-6768c854e9074a8aa0a36eb51283fdf3
Source noteuspto-grants-2009_05