反应详情

To a solution of N-methylbenzylamine (21 g) in methanol (50 ml), a solution of 6-(2,3-epoxypropoxy)carbostyril (4.4 g) in methanol (70 ml) is added dropwise over a period of 30 minutes under refluxing with heat. After the addition, the mixture is further heated with refluxing for 2 hours. The reaction mixture is concentrated under reduced pressure, and the resulting residue is purified by silica gel column chromatography (solvent; methanol:chloroform=1:100-1:25) and recrystallized from ethanol to give 6-[3-(N-methyl-N-benzylamino)-2-hydroxypropoxy]carbostyril (5 g), as white powder, m.p. 129°-132° C.

1. temperatureunder refluxing
2. temperaturewith heat
3. additionAfter the addition
4. temperaturethe mixture is further heated
5. temperaturewith refluxing for 2 hours
6. concentrationThe reaction mixture is concentrated under reduced pressure
7. customthe resulting residue is purified by silica gel column chromatography (solvent; methanol:chloroform=1:100-1:25)
8. customrecrystallized from ethanol