Potassium Iodide → HCID 71510469, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]-1-(4-{4-[5-(2,6-difluoro-3-hydroxyphenyl)-4,5-dihydro-1,2-oxazol-3-yl]-1,3-thiazol-2-yl}piperidin-1-yl)ethanone (1.82 g) and potassium carbonate (657 mg) in N,N-dimethylformamide (15 ml) are added, at room temperature, potassium iodide (289 mg) and 3-bromoprop-1-yne (755 mg)) (80 wt % in toluene). The reaction mixture is stirred at 80° C. for 4 h. Then the mixture is admixed with saturated aqueous solution of ammonium chloride and extracted with ethyl acetate. The combined organic phases are dried over sodium sulphate and concentrated. Purification by column chromatography gives 2-[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]-1-[4-(4-{5-[2,6-difluoro-3-(prop-2-yn-1-yloxy)phenyl]-4,5-dihydro-1,2-oxazol-3-yl}-1,3-thiazol-2-yl)piperidin-1-yl]ethanone, (1.68 g).

Provenance & Evidence