Pyrrolidone carboxylic acid → HCID 66750924, compound

Participants

Reaction Steps

A mixture of 1-(2-tert-butylphenyl)piperazine dihydrochloride obtained in Reference Example 1 (1.00 g, 3.43 mmol), DL-pyroglutamic acid (0.49 g, 3.78 mmol), triethylamine (0.73 g, 7.20 mmol), EDCI (0.72 g, 3.78 mmol) and HOBt (0.58 g, 3.78 mmol) in acetonitrile (30 mL) was stirred at room temperature for 16 h. The reaction mixture was concentrated under reduced pressure and the resulting residue was partitioned between ethyl acetate and 10% sodium hydrogen carbonate solution. The resulting white precipitate was collected by filtration and washed with diethyl ether to afford the title compound (1.03 g, 91%) as a off-white solid, mp 290° C.

Provenance & Evidence