50848-67-4

Upstream product

• 50848-66-3 7,4'-dimethoxy-5-hydroxy-6-iodoflavone 
• 77-78-1 dimethyl sulfate 
• 90-24-4 2-hydroxy-4,6-dimethoxyacetophenone 
• 76288-41-0 1-(4'-methoxyphenyl)-3-(2''-hydroxy-3'',6''-dimethoxyphenyl)-1,3-propanedione 
• 100-07-2 4-methoxy-benzoyl chloride 
• 83171-42-0 4,6-dimethoxy-2-(4'-methoxybenzoyloxy)acetophenone 
• 5631-70-9 4',5,7-trimethoxyflavone 
• 5128-44-9 5-hydroxy-7-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one 

Downstream Products

• 28442-04-8 robustaflavone hexamethyl ether 
• 674367-92-1 5,7-Dimethoxy-2-(4-methoxy-phenyl)-6-((E)-3-methyl-buta-1,3-dienyl)-chromen-4-one 
• 49620-13-5 robustaflavone 
• 220906-13-8 6-(2-methoxyphenyl) apigenin trimethyl ether 

Relevant academic research and scientific papers

COMPOSITIONS AND METHODS FOR POTENTIATING ANTIBIOTIC ACTIVITY

[205] The present invention provides compounds that potentiate the activity of antibiotic agents, particularly quinolones such as norflaxin. The invention further provides compositions, e.g., pharmaceutical compositions, comprising the inventive compounds. The invention also provides compositions comprising an antibiotic (e.g., a quinolone) and a compound that potentiates activity of the antibiotic. The invention further provides methods of treating a subject comprising administering any of the inventive compounds or compositions to the subject. The invention also provides screening methods to identify compounds that potentiate the activity of an antibiotic, e.g., a quinolone.

Total synthesis of robustaflavone, a potential anti-hepatitis B agent

Robustaflavone, a naturally occurring compound, is an inhibitor of hepatitis B virus replication in vitro. Robustaflavone is a biflavanoid composed of two units of apigenin (5,7,4'-trihydroxyflavone) joined via a biaryl linkage between the 6-position of one unit and the 3'-position of the other (I6,II3'-biapigenin). The natural material was isolated from the seed- kernels of Rhus succedanea. To provide ready access to sufficient quantities of material for continued biological studies, as well as to provide a general route for the preparation of structural analogues, a total synthesis of robustaflavone was pursued. The total synthesis was approached by constructing apigenin ethers containing functionalities at the 6- and 3'- positions which could be cross-coupled using transition metal catalysis. Key steps of the synthesis included development of a regioselective iodination of an apigenin derivative at the 6-position. Also key was the formation of an apigenin 3'-boronate using a palladium-catalyzed exchange of the corresponding 3'-iodide with a diboron reagent. Finally, identification of appropriate reaction conditions for Suzuki coupling to form the sterically congested 6-3''' biaryl bond of robustaflavone provided access to the desired biflavanoid system. This work represents the first total synthesis of robustaflavone.