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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1021244Generated: October 31, 2026

4-Chloropyrimidine hydrochloride → 4-{4-[3-({[Tert-butyl(dimethyl)silyl]oxy}methyl)-2-fluorophenyl]piperazin-1-yl}pyrimidine

https://huagongshe.com/reaction/1021244

Reaction equation

Participants

RoleNameHCIDCharge
Reactant4-Chloropyrimidine hydrochlorideHCID 21922556—
Reactant1-[3-({[tert-Butyl(dimethyl)silyl]oxy}methyl)-2-fluorophenyl]piperazineHCID 86686202—
SolventIsopropanolHCID 3776—
Product4-{4-[3-({[Tert-butyl(dimethyl)silyl]oxy}methyl)-2-fluorophenyl]piperazin-1-yl}pyrimidineHCID 8668621397.8%

Reaction Conditions

Temperature60 °C

Reaction Steps

1-[3-({[tert-Butyl(dimethyl)silyl]oxy}methyl)-2-fluorophenyl]piperazine (355 mg) was mixed with IPA (4.5 ml), and 4-chloro-pyrimidine hydrochloride (150 mg) and TEA (302 mg) were added thereto, followed by stirring at 60° C. overnight. The reaction mixture was cooled to room temperature and then concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (MeOH/CHCl3) to obtain 4-{4-[3-({[tert-butyl(dimethyl)silyl]oxy}methyl)-2-fluorophenyl]piperazin-1-yl}pyrimidine (391 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08716470B2
Source datasetuspto-grants-2014_05
ORD IDord-10d77c780e0e491cad34ab2de3d87ab3
Source noteuspto-grants-2014_05