Triethylamine → HCID 66811752, compound

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Reaction Steps

In CH3CN, 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) (0.5 g, 1.17 mmol). While stirring the solution, Et3N (0.2 g, 2.0 mmol) and TMSCN (0.47 g, 4.70 mmol) were slowly added dropwise thereto, and the resultant 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 CH2Cl2, 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 (MC/EA, 2/1) to obtain the desired compound, 2-(2-cyano-pyridin-5-yl)-7-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine (Compound 123) (0.37 g, 72%) and 2-(6-cyano-pyridin-5-yl)-7-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidine (Compound 124) (0.12 g, 24%).

Provenance & Evidence