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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1619615Generated: November 1, 2026

Hydrochloric Acid → 5-Chloro-2-fluoro-4-({3-[2-(piperazin-1-yl)pyridin-4-yl]-4'-(trifluoromethyl)biphenyl-4-yl}oxy)-N-(pyrimidin-4-yl)benzenesulfonamide hydrochloride salt

https://huagongshe.com/reaction/1619615

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
ReactantTert-butyl 4-{4-[4-(2-chloro-4-{[(2,4-dimethoxybenzyl)(pyrimidin-4-yl)amino]sulfonyl}-5-fluorophenoxy)-4'-(trifluoromethyl)biphenyl-3-yl]pyridin-2-yl}piperazine-1-carboxylateHCID 58042259—
SolventMethanolHCID 887—
Solvent1,4-DioxaneHCID 31275—
Product5-Chloro-2-fluoro-4-({3-[2-(piperazin-1-yl)pyridin-4-yl]-4'-(trifluoromethyl)biphenyl-4-yl}oxy)-N-(pyrimidin-4-yl)benzenesulfonamide hydrochloride saltHCID 56601784163.6%

Reaction Steps

A 4M solution of hydrogen chloride in 1,4-dioxane (10 mL) was added to a solution of tert-butyl 4-(4-(4-(2-chloro-4-(N-(2,4-dimethoxybenzyl)-N-(pyrimidin-4-yl)sulfamoyl)-5-fluorophenoxy)-4′-(trifluoromethyl)biphenyl-3-yl)pyridin-2-yl)piperazine-1-carboxylate (Preparation 109, 310 mg, 0.332 mmol) in methanol (2 mL). The reaction mixture was stirred at room temperature for 3 hours and then concentrated in vacuo. The residue was purified by reverse phase chromatography (acetonitrile/water with 0.1% formic acid) to afford the title compound (196 mg, 82%) as a white solid.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08772293B2
Source datasetuspto-grants-2014_07
ORD IDord-829a5e80c883412bb0460d888b363fe7
Source noteuspto-grants-2014_07