3-Thiocresol → HCID 66697853, compound

Participants

Reaction Conditions

Reaction Steps

A solution of ethyl 1-(2-fluoropyridin-3-yl)-5-{[(trifluoromethyl)sulfonyl]oxy}-1H-pyrazole-3-carboxylate (575 mg), 3-methylbenzenethiol (224 mg) and sodium carbonate (238 mg) in toluene (7.5 mL) was sufficiently deaerated, tris(dibenzylideneacetone)dipalladium(0) (41 mg) and 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (52 mg) were added, and the mixture was further deaerated. Under an argon atmosphere at 130° C., the mixture was stirred for 28 hr and allowed to cool to room temperature. Ethyl acetate was added and the mixture was filtered through a basic silica gel pad. The filtrate was concentrated under reduced pressure, and the obtained residue was purified by silica gel column chromatography (eluent:hexane-ethyl acetate=9:1→2:1) to give the title compound as a crude yellow oil (yield 334 mg).

Provenance & Evidence