反应详情

A mixture of 2.84 grams of 1H-benzimidazole-1-butanamine and 3.11 grams of 1-[4-(2-amino-2-oxoethyl)phenoxy]-2,3-epoxypropane in 50 ml of 90% methanol was heated at reflux for 22 hours. The solvent was evaporated and the residue was triturated with ether to give an off-white solid. This was chromatographed on a silica gel column using methanol. The fractions containing the desired product were determined by thin-layer chromatography and combined. The solvent was then evaporated to give N-{3-[4-(2-amino-2-oxoethyl)phenoxy]-2-hydroxypropyl}-1H-benzimidazole-1-butanamine as an off-white solid melting at about 119°-123° C. This compound has the following structural formula: ##STR13##

1. temperaturewas heated
2. temperatureat reflux for 22 hours
3. customThe solvent was evaporated
4. customthe residue was triturated with ether
5. customto give an off-white solid
6. customThis was chromatographed on a silica gel column
7. additionThe fractions containing the desired product
8. customThe solvent was then evaporated