Triethylamine → tert-Butyl 4-(bromoacetyl)piperazine-1-carboxylate

Participants

Reaction Steps

To a stirring solution of bromoacetyl bromide (29.8 g, 148 mmol) in THF (250 mL) at 0° C. was added via an addition funnel a solution of Boc-piperazine (25 g, 134 mmol) and triethylamine (14.9 g, 148 mmol) in THF (75 mL). After 1 h, a few grams of ice were added and the mixture was diluted with ethyl acetate and cold water. The layers were separated and the organic phase was washed with 1 M aq. citric acid, brine, satd aq. NaHCO3 and again with brine. The organic phase was then dried with MgSO4, filtered, and concentrated in vacuo to give 38.2 g (93%) of an off-white powder.

Provenance & Evidence