反应详情

The mixture of 2-bromo-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (320 mg, 0.9 mmol), tert-butylamine (0.5 mL, 4.5 mmol) and HATU (684 mg, 1.8 mmol) in 50 mL of dry THF was stirred for 4 hours at room temperature. The reaction mixture was evaporated to dryness, then the residue was suspended in 50 mL of 0.5 N HCl, product extracted with ethyl acetate (50 mL×3), dried with sodium sulfate, filtered and concentrated to give 2-bromo-N-tert-butyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide (258 mg, crude), material used in the next step without further purification. LCMS: (M+H)+=297/299; (M+Na)+=319/321.

1. customThe reaction mixture was evaporated to dryness
2. extractionproduct extracted with ethyl acetate (50 mL×3)
3. dry with materialdried with sodium sulfate
4. filtrationfiltered
5. concentrationconcentrated