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Paper | Special issue | Vol 82, No. 1, 2010, pp.377-396
Published online, 10th May, 2010
DOI: 10.3987/COM-10-S(E)9
Synthesis of Novel 1-Hydroxyquinolones with High Anti-Toxoplasma Activity

Lutz F. Tietze* and Ling Ma

*Institute of Organic and Biomolecular Chemistry, Georg-August-University, Tammannstr. 2, D-37077 Göttingen, Germany

Abstract

All for the treatment of malaria and toxoplasmosis the novel hydroxyquinolones 25 were prepared by reaction of aniline and hydroxyaniline, respectively and the β-ketoesters 10a-c. As products the quinolones 8 and 15, respectively were obtained. Benzylation, oxidation and hydrogenation then led to the desired substances. Compound 2 has a similar anti-malaria activity as the approved drug Atovaquone.