Synthesis of Gerfelin and Related Analogous Compounds
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Gerfelin, an inhibitor of human geranylgeranyl diphosphate (GGPP) synthase that has been isolated from a culture broth of <I>Beauveria felina</I> QN22047, was synthesized in 4 and 3 steps starting from 2,4-dihydroxy-6-methylbenzoic acid and 3,4,5-trihydroxytoluene, respectively. An effective ligand, 2-(di-<I>tert</I>-butylphosphino)biphenyl, was used in the palladium-catalyzed diaryl ether-forming reaction. Five analogous compounds of gerfelin were also synthesized for a study of the structure-activity relationship.
- Agricultural and Biological Chemistry
Agricultural and Biological Chemistry 70(10), 2523-2528, 2006-10-23
Japan Society for Bioscience, Biotechnology, and Agrochemistry