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8,8′-Biflavone Synthesis

The work of Moritz Klischan et al. dealt with the synthesis of a library of non-natural 8,8'-biflavones. To overcome the problems of chemoselectivity, he synthesized the key intermediate acetophenone dimer via a one-step oxidative coupling process. Finally, the synthesis could be performed on an 8 g scale without column chromatographic isolation, synthesizing 14 flavones and 13 biflavones according to the established protocol.

Additionally, antiproliferative activity of the compounds against T. gondii and selective cytotoxicity against human cancer cell lines (HeLa) was demonstrated, with the biflavones exhibiting higher activity than their monomers.

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