Synthesis and antimalarial activity of febrifugine derivatives

Y. Takeuchi, M. Koike, K. Azuma, H. Nishioka, H. Abe, H. S. Kim, Y. Wataya, T. Harayama

Research output: Contribution to journalArticlepeer-review

22 Citations (Scopus)


The regioisomers (2a,b) of the piperidine ring of febrifugine (1a) and isofebrifugine (1b) were synthesized from 4-allyl-3-piperidone (5). Reduction of 5 afforded a mixture of the trans and cis alcohols (6a,b) without diastereoselectivity; this result differentiated it from the reduction of 2-allyl-3-piperidone (14). The antimalarial di-activity of 2a,b and related compounds was tested.

Original languageEnglish
Pages (from-to)721-725
Number of pages5
JournalChemical and Pharmaceutical Bulletin
Issue number6
Publication statusPublished - 2001


  • Antimalarial activity
  • Febrifugine
  • Structure-activity relationship
  • Synthesis

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery


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