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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1485007Generated: November 1, 2026

Cesium carbonate → 4-(2-Chloro-pyridin-3-ylamino)-N-cyclopropylmethyl-2-trifluoromethyl-benzenesulfonamide

https://huagongshe.com/reaction/1485007

Reaction equation

Participants

RoleNameHCIDCharge
ReactantCesium carbonateHCID 10796—
Reactant2-Chloro-3-pyridylamineHCID 80528—
ReactantBinap, (A+-)-HCID 634876—
Reactant4-bromo-N-(cyclopropylmethyl)-2-(trifluoromethyl)benzenesulfonamideHCID 24948367—
Catalystpalladium(II) acetateHCID 167845—
SolventTolueneHCID 1140—
Product4-(2-Chloro-pyridin-3-ylamino)-N-cyclopropylmethyl-2-trifluoromethyl-benzenesulfonamideHCID 24946708—

Reaction Steps

A mixture of 4-Bromo-N-cyclopropylmethyl-2-trifluoromethyl-benzenesulfonamide (150 mg), Pd(OAc)2 (9.5 mg), BINAP (26 mg), cesium carbonate (164 mg) and 2-Chloro-pyridin-3-ylamine (108 mg) in 15 ml toluene was relaxed for 12 hours. The reaction mixture was eluted through a silica bed with Toluene and then with PE:EtOAc (1:1). The toluene fraction was discarded and the solvent of the PE:EtOAc fraction was removed under reduced pressure. The crude product was purified by Combiflash (linear gradient PE-THF). Yield 25 mg, 15%.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09422235B2
Source datasetuspto-grants-2016_08
ORD IDord-19647fe899654b119e212658bcacbbd1
Source noteuspto-grants-2016_08