反应详情

4-(5-Amino-1-benzenesulfonyl 1H-pyrrolo[2,3-b]pyridine-4-ylamino)-piperidine-1-carboxylic acid tert-butyl ester (1.00 g, 2.12 mmol), isobutyryl chloride (225 mg, 2.12 mmol) and triethylamine (590 μL, 4.24 mmol) in DCM (15 mL) were stirred at ambient temperature for 2 hours. The mixture was diluted with DCM, washed with a saturated sodium hydrogen carbonate solution, water and brine, dried through a phase separator and concentrated under vacuum affording 4-(1-benzenesulfonyl-5-isobutyrylamino-1H-pyrrolo[2,3-b]pyridine-4-ylamino)-piperidine-1-carboxylic acid tert-butyl ester as a brown residue which was used for the next step without further purification. LCMS (Method B, ESI): RT=3.77 min, m+H=542.36.

1. washwashed with a saturated sodium hydrogen carbonate solution, water and brine
2. customdried through a phase separator
3. concentrationconcentrated under vacuum