Bicyclo[2.2.1]heptane-1-methanesulfonic acid, 7,7-dimethyl-2-oxo-, (1S)- → (6-Bromo-imidazo[1,2-a]pyrazin-8-yl)-[4-(1-methyl-piperidin-4-yl)-phenyl]-amine

Participants

Reaction Steps

A solution of 6,8-dibromoimidazo[1,2-a]pyrazine (500 mg, 1.8 mmol), 4-(1-methylpiperidin-4-yl)benzenamine (376 mg, 1.98 mmol) and CSA (356 mg, 1.53 mmol) in iPrOH (30 mL) was stirred at 90° C. overnight. The solvent was evaporated. The residue was dissolved in DCM (30 mL), NaHCO3 solution (10 mL) was added to adjust pH=8. The organic layer was dried over Na2SO4 and evaporated. The residue was purified through a silica-gel column (ethyl acetate:petroleum ether=1:1) to afford the desired product as a yellow solid (400 mg, 58% yield).

Provenance & Evidence