反应详情

4-(4-Benzylpiperazin-1-yl)-1H-pyrrolo[2,3-b]pyridin-3-amine (0.35 g, 1.14 mmol, see Example 25) was placed in DCM (2 mL) and pyridine (1 mL). Acetic anhydride (0.129 mL, 1.37 mmol) was then added, and the reaction was stirred at room temperature for 1 hour. The reaction was then diluted with MeOH (5 mL), and 3M LiOH (0.5 mL) was added. The reaction was stirred for 10 minutes and then poured into saturated Na2CO3 and extracted into DCM. The organic fractions were combined, dried, filtered and concentrated to give a crude residue that was purified by column chromatography (500:8-500:20 DCM:MeOH) to give N-(4-(4-benzylpiperazin-1-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetamide (0.35 g, 88.0% yield).

1. additionwas added
2. stirringThe reaction was stirred for 10 minutes
3. extractionextracted into DCM
4. customdried
5. filtrationfiltered
6. concentrationconcentrated
7. customto give a crude residue that
8. customwas purified by column chromatography (500:8-500:20 DCM:MeOH)