Befuraline Explained

Befuraline (DIV-154) is a psychoactive drug and member of the piperazine chemical class which was developed in Germany in the 1970s.^[1] Befuraline has stimulant and antidepressant effects and has seen some use in Germany and France, although it has never become widely used.^[2] Befuraline's active metabolite benzylpiperazine is likely to contribute to its effects.

Synthesis

A one-step coupling between coumarilic acid (benzofuran-2-carboxylic acid) [496-41-3] (1) and benzylpiperazine (BzP) (2) gives an amide, and hence Befuraline (3).

See also

• Substituted piperazine
• Fipexide
• Piberaline

Notes and References

1. Boksay IJ, Popendiker K, Weber RO, Söder A . Synthesis and pharmacological activity of befuraline (N-benzo[b]furan-2-ylcarbonyl-N'-benzylpiperazine), a new antidepressant compound . Arzneimittel-Forschung . 29 . 2 . 193–204 . 1979 . 582130 .
2. Gastpar M, Gastpar G, Gilsdorf U . Befuraline, its safety and efficacy in depressed inpatients . Pharmacopsychiatry . 18 . 6 . 351–5 . November 1985 . 4089015 . 10.1055/s-2007-1017396 . 9322026 .