In a vial, N-[(4-bromophenyl)methyl]-N-tert-butyl-1-phenylmethanesulfonamide (186 mg; 0.47 mmol), palladium(II) acetate (5 mg, 0.023 mmol), 2-dicyclohexylphosphino-2′,6′-di-i-propoxy-1,1′-biphenyl (22 mg, 0.047 mmol) sodium tert-butoxide (61 mg, 0.61 mmol) were weighed out and the vial was purged with nitrogen. 1,4-Dioxane (3 mL) and 1-piperazin-1-ylethanone (78 mg, 0.61 mmol) were then added and the reaction was stirred at 100° C. for 16 hours. The reaction was filtered through diatomaceous earth, concentrated and purified by preparative reverse phase HPLC to yield 141 mg of N-(4-(4-acetylpiperazin-1-yl)benzyl)-N-tert-butyl-1-phenylmethanesulfonamide. 1H NMR (400 MHz, DMSO) δ 7.47-7.33 (m, 5H), 7.27-7.16 (m, 2H), 6.96-6.83 (m, 2H), 4.41 (s, 2H), 4.16 (s, 2H), 3.62-3.49 (m, 4H), 3.19-3.09 (m, 2H), 3.09-2.95 (m, 2H), 2.03 (s, 3H), 1.33 (s, 9H); LCMS (m/z) ES+ 444.1 [M+1]+.
