反应详情

To 2,6-dichloro-N-{1-cyano-2-[2-(2,6-dichlorophenyl)-6-quinolinyl]ethyl}benzamide 58 (0.358 g) in toluene (5 ml) are added trimethylsilyl azide (184 μl) and dibutyltin oxide (17 mg). The solution is heated at reflux overnight, then evaporated under vacuum. The resulting residue is purified twice over silica gel using one time CH2Cl2/CH3OH 85/15 as eluent and the second time CH2Cl2/(CH3OH-10% NH4OH) 85/15 to give 2,6-dichloro-N-[2-[2-(2,6-dichlorophenyl)-6-quinolinyl]-1-(1H-tetraazol-5-yl)ethyl]benzamide 126.

1. temperatureThe solution is heated
2. temperatureat reflux overnight
3. customevaporated under vacuum
4. customThe resulting residue is purified twice over silica gel using one time CH2Cl2/CH3OH 85/15 as eluent