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Note | Regular issue | Vol 75, No. 7, 2008, pp.1735-1743
Published online, 11th March, 2008
DOI: 10.3987/COM-08-11324
Synthesis of 6-Pyridylaminopurines

Luc Demange, Nassima Oumata, Julia Quinton, Serge Bouaziz, Olivier Lozach, Laurent Meijer, and Hervé Galons*

*INSERM U648, Université Paris Descartes, 4, avenue de l’Observatoire 75006 Paris, France

Abstract

An efficient synthesis of new 6-pyridinylaminopurines was developed based on Buchwald-Hartwig coupling reaction between aminopyridines and 2,6-dichloro-9-iso-propylpurine. The reaction was best carried out in the presence of a limited load of palladium acetate (4 %) as catalyst, racemic 2,2’-bis(diphenylphosphanyl)-1,1’-binaphtyl (8 %) as ligand and potassium tert-butoxide as base. Rising the load of catalyst, or using other catalysts and bases led to the development of side reactions.