反应详情

A mixture of 540 mg of 3-(4-cyanobutyl)-2-(3-pyridyl)indole, 173 mg of sodium azide, 142 mg of ammonium chloride and 5 mg of lithium chloride in 2 ml of DMF is heated at 120° overnight. After cooling the mixture is filtered and the filtrate diluted with ca. 25 ml of water. After the pH is adjusted to 10-11 with 3N NaOH, the solution is washed with ether to remove unreacted nitrile. The aqueous phase is adjusted to pH 5-6 with 2N HCl and extracted with ether. The ether extract is washed with water, dried over MgSO4 and concentrated in vacuo. The residue is purified to give 3-[4-(5-tetrazolyl)-butyl]-2-(3-pyridyl)indole.

1. temperatureis heated at 120° overnight
2. temperatureAfter cooling the mixture
3. filtrationis filtered
4. additionthe filtrate diluted with ca. 25 ml of water
5. washthe solution is washed with ether
6. customto remove unreacted nitrile
7. extractionextracted with ether
8. extractionThe ether extract
9. washis washed with water
10. dry with materialdried over MgSO4
11. concentrationconcentrated in vacuo
12. customThe residue is purified