Journal
TETRAHEDRON
Volume 72, Issue 40, Pages 6118-6126Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2016.08.043
Keywords
Peroxide chemistry; Antimalarial; Reductive amination; Chemoselective reduction; Medicinal chemistry
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Funding
- European Commission FP6 [EU 018834]
- Medicines for Malaria Venture (MMV)
- Engineering and Physical Sciences Research Council [EP/K039687/1] Funding Source: researchfish
- EPSRC [EP/K039687/1] Funding Source: UKRI
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An efficient route to the synthesis of potent antimalarial aryloxy 1,2,4,5-tetraoxanes is described that permits parallel synthesis for Structure Activity Relationship (SAR) investigations. Brief details of the in vitro and in vivo antimalarial evaluation are included which enables identification of antimalarial leads for further development. Also described is an improved approach to the synthesis of a selected late lead compound in just four or five synthetic steps from commercially available starting materials. (C) 2016 Published by Elsevier Ltd.
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