Journal
TETRAHEDRON LETTERS
Volume 52, Issue 30, Pages 3909-3911Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2011.05.088
Keywords
Synthesis; Benzoxaborole; Antimalarial therapeutics; Malaria; Plasmodium falciparum
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Efficient synthesis is essential for antimalarial therapeutics. A four-step route has been established for the synthesis of 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole 1 that is a potent new class boron-containing antimalarial agent in preclinical development with IC(50) = 26 nM against the malaria parasite Plasmodium falciparum. (C) 2011 Elsevier Ltd. All rights reserved.
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