Potassium Carbonate → tert-butyl (3R)-4-[2-(3-cyano-4-fluorophenyl)-2-oxoethyl]-3-(hydroxymethyl)piperazine-1-carboxylate

Participants

Reaction Steps

To a solution of 5-(bromoacetyl)-2-fluorobenzonitrile (13.1 g, 0.054 mol) in DMF (160 mL) was added tert-butyl (3R)-3-(hydroxymethyl)piperazine-1-carboxylate (13.1 g, 0.065 mol) and K2CO3 (11.77 g, 0.075 mol), and the mixture was stirred at r.t for 3 h. The mixture was washed with water, and extracted with EtOAc. The organic layer was washed with brine dried over Na2SO4 and concentrated in vacuum to give the desired product, which can be used for next step without further purification.

Provenance & Evidence