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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 557084Generated: October 30, 2026

Pyridine → 4-(4-Chloro-phenyl)-3-methoxycarbonylmethyl-piperazine-1-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/557084

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPyridineHCID 1049—
Reactant4-Chlorophenylboronic acidHCID 74299—
ReactantMethyl 4-Boc-piperazine-2-acetateHCID 2756816—
CatalystCupric acetateHCID 8895—
SolventDichloromethaneHCID 6344—
Product4-(4-Chloro-phenyl)-3-methoxycarbonylmethyl-piperazine-1-carboxylic acid tert-butyl esterHCID 66758668—

Reaction Steps

4-Chlorophenyl boronic acid (1.08 g, 6.97 mmol) and 3-methoxycarbonylmethyl-piperazine-1-carboxylic acid tert-butyl ester (0.9 g, 3.48 mmol) were dissolved in dichloromethane. To this mixture was added copper acetate (0.63 g, 3.48 mmol), 4 Å molecular sieves and pyridine (0.56 mL, 6.97 mmol) and the reaction mixture was stirred at room temperature for 72 h. The reaction mixture was concentrated in vacuo and dissolved in ethyl acetate, filtered through celite and concentrated. The crude product was purified using gradient elution from hexane/ethyl acetate (5%) to hexane/ethyl acetate (20%). ESI-MS m/z: 369 (M+1), UV retention time: 2.97 min.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08058287B2
Source datasetuspto-grants-2011_11
ORD IDord-5061cc2b504e4a00b6ade102f85b0527
Source noteuspto-grants-2011_11