Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 645461Generated: October 29, 2026

Potassium Carbonate → (R)-1-[4-(2'-Difluoromethyl-biphenyl-3-yl)-piperazin-1-yl]-2-hydroxy-4-methyl-pentan-1-one

https://huagongshe.com/reaction/645461

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPotassium CarbonateHCID 11430—
Reactant2-[2-(Difluoromethyl)phenyl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolaneHCID 59264588—
Reactant1-[4-(3-Chloro-phenyl)-piperazin-1-yl]-2-hydroxy-4-methyl-pentan-1-oneHCID 68689983—
CatalystHCID 178418397HCID 178418397—
SolventWaterHCID 962—
SolventAcetonitrileHCID 6342—
SolventAcetonitrile--water (1/1)HCID 18373917—
Product(R)-1-[4-(2'-Difluoromethyl-biphenyl-3-yl)-piperazin-1-yl]-2-hydroxy-4-methyl-pentan-1-oneHCID 11957763—

Reaction Conditions

Temperature150 °C

Reaction Steps

2-(2-Difluoromethyl-phenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (34 mg, 0.11 mmol), 1-[4-(3-Chloro-phenyl)-piperazin-1-yl]-2-hydroxy -4-methyl-pentan-1-one (34 mg, 0.13 mmol), Pd(Ph3P)4 (1.3 mg, 10 μmol), K2CO3 (30.4 mg, 0.22 mmol), CH3CN (900 μL), and H2O (100 μL) were sealed in a microwave vessel and heated by microwave irradiation at 150° C. for 10 minutes. The reaction was filtered and purified by reverse phase HPLC (10%-99% CH3CN (0.035% TFA)/H2O (0.05% TFA)) to give 2. LCMS: m/z 403.7 (M+H)+ at 3.72 minutes (10% -99% CH3CN/H2O), (10%-99% CH3CN (0.035% TFA)/H2O (0.05% TFA)).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07705002B2
Source datasetuspto-grants-2010_04
ORD IDord-aa89e2b9cff64693ada3630dff07c6c4
Source noteuspto-grants-2010_04