Diisopropylethylamine → 1-[4-(8-Amino-1-iodo-imidazo[1,5-a]pyrazin-3-yl)-piperidin-1-yl]-2-dimethylamino-ethanone

Participants

Reaction Steps

To a stirred mixture of 1-iodo-3-piperidin-4-yl-imidazo[1,5-a]pyrazin-8-ylamine (1.000 g, 2.91 mmol) and dimethylamino-acetyl chloride (0.38967 g, 3.20 mmol) in DMF (10.00 mL) was added DIEA (2.58 mL, 14.57 mmol) at 0° C. The resulting mixture was stirred at rt. overnight. The mixture was diluted with sat. aq. NaHCO3 and extracted with DCM (50 ml×3). The extracts were combined, dried (Na2SO4). Solvent was then removed under reduced pressure and the resulting residue was used for next step without further purifications. MS (ES+): m/z 428.74 [MH+].

Provenance & Evidence