Phosphorus oxychloride → HCID 86641150, compound

Participants

Reaction Steps

In POCl3, dissolved was 3-[7-{3-(Cyclopropylmethoxy)-4-(difluoromethoxy)phenyl}-[1,2,4]triazolo[1,5-a]pyri midine-2-yl]-pyridine-N-oxide (Compound 102) (2.7 g, 6.347 mmol), and the mixture was heated under reflux. The solvent was distilled under reduced pressure, and NaHCO3(aq.) was added to the residue. The mixture was extracted three times with EA, and the extract was washed twice with brine, dried over MgSO4, filtered and evaporated under reduced pressure to remove solvent. The mixture was purified via silica gel column chromatography (hexane/EA, 1/1) to obtain the desired compound, 2-(6-chloropyridin-3-yl)-7-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine (Compound 104) (0.07 g, 30%) and 2-(2-chloropyridin-3-yl)-7-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine (Compound 105) (0.09 g, 38%).

Provenance & Evidence