Chemistry:Antrafenine

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Short description: Chemical compound
Antrafenine
Antrafenine.svg
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
MetabolismHepatic
ExcretionRenal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC30H26F6N4O2
Molar mass588.554 g·mol−1
3D model (JSmol)
  (verify)

Antrafenine (Stakane) is a phenylpiperazine derivative drug invented in 1979.[1] It acts as an analgesic and anti-inflammatory drug with similar efficacy to naproxen,[2] but is not widely used as it has largely been replaced by newer drugs.

Synthesis

Thieme Synthesis:[1] Patents:[3][4][5]

Method E: The reaction between 2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethanol [40004-29-3] (1) and Isatoic anhydride [118-48-9] (2) goes on to give 4-(3-(Trifluoromethyl)phenyl)piperazine-1-ethyl 2-aminobenzoate [51941-08-3] (3).

Method G: Alkylation with 4-chloro-7-(trifluoromethyl)quinoline [346-55-4] (4) completed the synthesis of antrafenine (5).

See also

References

  1. 1.0 1.1 "Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates". Journal of Medicinal Chemistry 22 (5): 554–9. May 1979. doi:10.1021/jm00191a017. PMID 458805. 
  2. "A double blind study of antrafenine, naproxen and placebo in osteoarthrosis". European Journal of Rheumatology and Inflammation 6 (2): 209–11. 1983. PMID 6673985. 
  3. Don Pierre Rene Lucien Giudicelli, et al. U.S. Patent 4,017,623 (1977 to Synthelabo SA).
  4. Don Pierre Rene Lucien Giudicelli, et al. U.S. Patent 3,935,229 (1976 to Synthelabo SA).
  5. Don Pierre Rene Lucien Giudicelli, et al. U.S. Patent 3,953,449 (1976 to Synthelabo SA).