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Synthesis and antimalarial activity of febrifugine derivatives
1Faculty of Pharmaceutical Sciences, Okayama University, Japan. take@pharm.okayama-u.ac.jp
Chemical & Pharmaceutical Bulletin
|June 20, 2001
Abstract:
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 activity of 2a,b and related compounds was tested.