Formaldehyde → HCID 66936064, compound

Participants

Reaction Steps

To a solution of (2S,5S)-2,5-dimethyl-1-(phenylmethyl)piperazine (J. Med. Chem. 2006, 49, 716-726) (770 mg, 3.77 mmol) in dichloromethane (25 mL) at 0° C. was added formaldehyde (0.396 mL, 37% water solution, 5.28 mmol) followed by sodium triacetoxyborohydride (959 mg, 4.52 mmol). The reaction mixture was allowed to warm to room temperature and stirred for 2 h before being diluted with dichloromethane and washed with 1N NaOH solution. The organics were washed with brine, dried (MgSO4) and evaporated to yield (2S,5S)-1,2,5-trimethyl-4-(phenylmethyl)piperazine (782 mg, 95%). LCMS: (M+H)+: 219.1.

Provenance & Evidence