1-Methylpiperazine → Methyl 3-{[({6-fluoro-3'-[(4-methyl-1-piperazinyl)methyl]-3-biphenylyl}methyl)(methyl)amino]carbonyl}benzoate

Participants

Reaction Steps

To a solution of methyl 3-{[[(6-fluoro-3′-formyl-3-biphenylyl)methyl](methyl)amino]carbonyl}benzoate (0.18 g, 0.444 mmol) in DCM (4.4 mL) was added 1-methylpiperazine (0.0542 mL, 0.488 mmol), and NaBH(OAc)3 (0.141 g, 0.666 mmol). The mixture was stirred at room temperature for 17 h and then the reaction was quenched with H2O (˜1 mL). The organic layer was separated, dried over Na2SO4 and purified by CombiFlash chromatograph to afford the title compound 0.202 g (93%). LC-MS m/z 490 (M+H)+.

Provenance & Evidence