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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 333799Generated: October 30, 2026

Triethylamine → Methanesulfonic acid 3-chloro-4-[2-(2-chloro-pyridin-4-yl)-3,3,3-trifluoro-2-hydroxy-1-methyl-propyl]-benzyl ester

https://huagongshe.com/reaction/333799

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTriethylamineHCID 8471—
ReactantMethanesulfonyl chlorideHCID 31297—
Reactant3-(2-Chloro-4-hydroxymethyl-phenyl)-2-(2-chloro-pyridin-4-yl)-1,1,1-trifluoro-butan-2-olHCID 25254449—
SolventTetrahydrofuranHCID 8028—
SolventEthyl AcetateHCID 8857—
ProductMethanesulfonic acid 3-chloro-4-[2-(2-chloro-pyridin-4-yl)-3,3,3-trifluoro-2-hydroxy-1-methyl-propyl]-benzyl esterHCID 86629101—

Reaction Steps

To a solution of 3-(2-chloro-4-hydroxymethyl-phenyl)-2-(2-chloro-pyridin-4-yl)-1,1,1-trifluoro-butan-2-ol (50 mg, Example 112) in THF (1 mL) was added NEt3 (30 mg, 0.03 mL) under argon at −10° C. Methanesulfonyl chloride (18 mg, 0.01 mL) was added and the mixture was allowed to stir for 30 minutes. The reaction mixture was diluted with ethyl acetate and washed successively with sat. KHCO3 solution and brine. The organic layer was dried over Na2SO4 and evaporated to give the desired compound as light yellow, viscous oil that was used without further purification (53 mg). MS (m/e)=358.1 (MH+).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08883786B2
Source datasetuspto-grants-2014_11
ORD IDord-8833e721195043c89182c96d03c9ffb3
Source noteuspto-grants-2014_11