反应详情

A mixture of 9.8 grams of 1H-benzimidazole-2-propanamine and 12.16 grams of 1-[4-(2-amino-2-oxoethyl)phenoxy]-2,3-epoxypropane in 400 ml of 95% methanol was refluxed for 17 hours. The solvent was then evaporated under reduced pressure and the residue was chromatographed on a silica gel column packed in chloroform and eluted with solutions containing increasing percentages of methanol in chloroform. The fractions eluted with 30% methanol were combined and the solvent evaporated under reduced pressure. The solid residue was triturated with ether and then separated and dried at reduced pressure and room temperature to give N-{3-[4-(2-amino-2-oxoethyl)phenoxy]-2-hydroxypropyl}-1H-benzimidazole-1-propanamine melting at about 92°-96° C. This compound has the following structural formula: ##STR12##

1. temperaturewas refluxed for 17 hours
2. customThe solvent was then evaporated under reduced pressure
3. customthe residue was chromatographed on a silica gel column
4. washeluted with solutions
5. additioncontaining
6. temperatureincreasing percentages of methanol in chloroform
7. washThe fractions eluted with 30% methanol
8. customthe solvent evaporated under reduced pressure
9. customThe solid residue was triturated with ether
10. customseparated
11. customdried at reduced pressure and room temperature