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Synthesis 2001(5): 0699-0701
DOI: 10.1055/s-2001-12774
SHORTPAPER
© Georg Thieme Verlag Stuttgart · New York

Synthesis of 4-Aryl-1-(4-methylpiperazin-1-yl)phthalazines by Suzuki-type Cross-coupling Reaction

Sébastien Guery, Isabelle Parrot, Yveline Rival*, Camille G. Wermuth
Laboratoire de Pharmacochimie de la Communication Cellulaire, Faculté de Pharmacie, Université Louis Pasteur, UMR 7081 du CNRS, 74 route du Rhin, 67401 Illkirch Cedex, France
Fax: +33(3)90244310; e-Mail: rival@pharma.u-strasbg.fr;
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Publication History

Received 10 January 2001
Publication Date:
28 September 2004 (online)

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Abstract

Starting from the commercially available 1,4-dichlorophthalazine, a series of 4-aryl-1-(4-methylpiperazin-1-yl)phthalazines was prepared with good yields and under mild conditions by means of a nucleophilic aromatic substitution and a palladium-catalyzed Suzuki cross-coupling.

Key words

1,4-dichlorophthalazine - Suzuki cross-coupling - palladium(II) catalyst - 4-aryl-1-(4-methylpiperazinyl)phthalazines - 5-HT3 ligands