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Synthesis 2007(3): 367-374  
DOI: 10.1055/s-2006-958963
PAPER
© Georg Thieme Verlag Stuttgart · New York

Synthesis of 8-Substituted Pyrazolo[1,5-a]-1,3,5-triazine Derivatives by Palladium-Catalyzed Cross-Coupling Reactions

Florence Popowycza, Philippe Bernardb, Pierre Raboissonb, Benoît Joseph*a
a Laboratoire de Chimie Organique 1, UMR-CNRS 5181, Université Claude Bernard - Lyon 1, CPE - Bâtiment 308, 43 Boulevard du 11 Novembre 1918, 69622 Villeurbanne cedex, France
Fax: +33(4)72431214; e-Mail: benoit.joseph@univ-lyon1.fr;
b Greenpharma SA, 3 Allée du Titane, 45100 Orléans, France
Further Information

Publication History

Received 5 September 2006
Publication Date:
21 December 2006 (online)

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Abstract

8-Substituted pyrazolo[1,5-a]-1,3,5-triazine derivatives 6 were prepared from the corresponding 8-iodopyrazolo[1,5-a]-1,3,5-triazines 5 through palladium-catalyzed cross-coupling reactions. Several bioisosteres of hypoxanthine drugs 2 were then prepared by final nucleophilic aromatic substitution.

Key words

purine - bioisosteres - pyrazolo[1,5-a]-1,3,5-triazine - palladium

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