反应详情

350 mg of methyl(10-methoxymethyl-10H-pyrazino[2,3-b][1,4]benzothiazin-8-yl)acetothioimidate was dissolved in a solvent mixture of tetrahydrofuran (7 ml) with methanol (15 ml). After adding 0.5 ml of aniline, the resulting mixture was heated under reflux for 5 hours. Then the reaction mixture was brought back to room temperature. After distilling off the solvent under reduced pressure, the residue was purified by silica gel column chromatography (eluted with dichloromethane/methanol/aqueous ammonia) to thereby give 250 mg of the title compound as yellow crystals.

1. temperaturethe resulting mixture was heated
2. temperatureunder reflux for 5 hours
3. customwas brought back to room temperature
4. distillationAfter distilling off the solvent under reduced pressure
5. customthe residue was purified by silica gel column chromatography (eluted with dichloromethane/methanol/aqueous ammonia)