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Paper | Regular issue | Vol 57, No. 5, 2002, pp.871-879
Published online, 1st January, 1970
DOI: 10.3987/COM-02-9463
Synthesis of 8-Substituted Xanthine Derivatives by Suzuki Cross-Coupling Reaction

Karl Vollmann and Christa E. Müller*

*Pharmaceutical Institute Poppelsdorf, University of Bonn, Kreuzbergweg 26, D-53115 Bonn, Germany

Abstract

A Suzuki cross-coupling reaction procedure was developed to prepare 8-substituted 3,7-dihydropurine-2,6-dione (xanthine) derivatives. 8-Halogen-substituted xanthines were reacted with phenyl- and styrylboronic acids. The best results were obtained using tetrakis(triphenylphosphine)palladium(0) and tripotassium phosphate in dimethylformamide. The developed procedure allows for a convergent synthesis of pharmacologically active 8-substituted xanthine derivatives.