Advanced Life Sciences, Inc.

Heping Zhang

Michael T Flavin

David E Zembower

Yuh-Meei Lin

Robustaflavone, intermediates and analogues thereof and a method for synthesizing the same are provided. The method involves constructing apigenin ethers containing functionalities at the 6- and 3&prime;-positions which could be cross-coupled using transition metal catalysis. The method also involves development of a regioselective iodination of an apigenin derivative at the 6-position, formation of an apigenin 3&prime;-boronate using a palladium-catalyzed exchange of the corresponding 3&prime;-iodide with a diboron reagent. Finally, Suzuki coupling to form the sterically congested 6-3&prime;&Prime; biaryl bond of robustaflavone provides access to the desired biflavanoid system. Robustaflavone intermediates and analogues may be used to prepare analogues of other biflavanoids such as hinokifavone, rhusflavone and succedaneaflavone.

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Elmhurst, IL, United States of America

Heping Zhang