Synthesis of Gerfelin and Related Analogous Compounds
- 23 October 2006
- journal article
- Published by Informa UK Limited in Bioscience, Biotechnology, and Biochemistry
- Vol. 70 (10), 2523-2528
- https://doi.org/10.1271/bbb.60287
Abstract
Gerfelin, an inhibitor of human geranylgeranyl diphosphate (GGPP) synthase that has been isolated from a culture broth of Beauveria felina 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-tert-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.Keywords
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