Potassium Carbonate → 1,1-Dimethylethyl 4-{[5'-(aminomethyl)-2'-fluoro-3-biphenylyl]methyl}-1-piperazinecarboxylate

Participants

Reaction Conditions

Reaction Steps

To two vials which each contained a solution of [(3-bromo-4-fluorophenyl)methyl]amine hydrochloric salt (0.601 g, 2.5 mmol) in p-dioxane/H2O (15/5 mL) was added {3-[(4-{[(1,1-dimethylethyl)oxy]carbonyl}-1-piperazinyl)methyl]phenyl}boronic acid (1.2 g, 3.75 mmol), Pd(PPh3)4 (145 mg, 0.125 mmol), and K2CO3 (1.38 g, 10 mmol). The mixture was heated with a microwave at 150° C. for 15 min. The organic layer of both vials was separated, combined, concentrated and purified by CombiFlash chromatograph to afford the title compound 1.98 g (99%). LC-MS m/z 400 (M+H)+.

Provenance & Evidence