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Nucleic Acids Symposium Series 2005 49(1):29-30; doi:10.1093/nass/49.1.29
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© 2005 Oxford University Press

Novel modified purine bases and nucleosides: new methodologies of synthesis and biological activity

Michal Hocek *

Centre for New Antivirals and Antineoplastics, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, CZ-16610 Prague 6, Czech Republic

Novel modified purine derivatives (bases or nucleosides) bearing C-substituents in position(s) 6, 2 and/or 8 were prepared by Pd- or Fe-catalyzed cross-coupling reactions of halopurines with organometallics. Reactions of di- and trihalopurines are regioselective and applicable to the synthesis of di- or trisubstituted purines bearing different substituents. Cross-coupling reactions of protected functionalized organometallics were used for the preparation of purines bearing functionalized C-substituents. Some of the title modified purine bases and nucleosides display cytostatic activity.


* e-mail: hocek{at}uochb.cas.cz


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