Triethylamine → HCID 66691794, compound

Participants

Reaction Steps

Phenyl chloroformate (200 μL, 1.57 mmol) was added dropwise to 1-(2,2,2-trifluoroethyl)piperidin-4-amine (400 mg, 1.57 mmol) dissolved in a mixed solvent of acetonitrile (3 mL) and dimethylacetamide (1 mL) at 0° C., followed by stirring at the same temperature for 1 hour, and 4-(2,5-difluorobenzylidene)piperidine hydrochloride (580 mg, 2.36 mmol) obtained in Example 34 (1) and Et3N (430 μL) were added thereto, followed by stirring at 60° C. overnight. Water was added to the reaction mixture, and after extraction with chloroform, the extract was washed with water and a saturated sodium chloride aqueous solution, and dried over anhydrous magnesium sulfate. After the desiccant was filtered off, the residue obtained by evaporation under reduced pressure was purified using medium pressure silica gel flash column chromatography (methanol:chloroform=1:50), thereby giving the title compound (110 mg, 17%) as a white solid.

Provenance & Evidence