反应详情

0.33 g of the above-obtained 3-aminomethylimidazo[5,1-b]-thiazole was dissolved in 10 ml of dichloromethane. To this solution, a mixture which had been prepared in advance by reacting 0.5 ml of formic acid with 0.5 ml of acetic anhydride at 50° C. for 10 minutes was added with stirring, and the resulting mixture was stirred at room temperature for an additional one hour. To the reaction solution was added 20 ml of a saturated aqueous solution of sodium hydrogencarbonate, and the organic layer was separated. The aqueous layer was extracted with dichloromethane (10 ml×2). The combined organic layers were dried over anhydrous magnesium sulfate, and concentrated to dryness under reduced pressure to give 0.338 g (yield 87%) of the title compound.

1. customTo this solution, a mixture which had been prepared in advance
2. customat 50° C.
3. customfor 10 minutes
4. additionwas added
5. stirringthe resulting mixture was stirred at room temperature for an additional one hour
6. customthe organic layer was separated
7. extractionThe aqueous layer was extracted with dichloromethane (10 ml×2)
8. dry with materialThe combined organic layers were dried over anhydrous magnesium sulfate
9. concentrationconcentrated to dryness under reduced pressure