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Synthesis 2011(19): 3115-3122  
DOI: 10.1055/s-0030-1260197
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

Efficient and Original Microwave-Assisted Suzuki-Miyaura Cross-Coupling Reaction in the 4H-Pyrido[1,2-a]pyrimidin-4-one Series

Youssef Kabri, Maxime D. Crozet, Rémi Szabo, Patrice Vanelle*
Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, Universités d′Aix-Marseille I, II et III - CNRS, UMR 6264, Laboratoire Chimie Provence, 27 Boulevard J. Moulin, 13385 Marseille Cedex 05, France
Fax: +33(4)86136822; e-Mail: patrice.vanelle@univmed.fr;
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Publication History

Received 18 May 2011
Publication Date:
01 September 2011 (online)

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Abstract

An efficient synthesis of new series of various 3-aryl, 3-heteroaryl, and 3-styryl-4H-pyrido[1,2-a]pyrimidin-4-ones by palladium-catalyzed Suzuki-Miyaura cross-coupling reactions using microwave irradiation is described. The coupling process is tolerant of electron-poor, electron-rich, and bulky boronic acid derivatives, and leads to the desired products in good yields.

Key words

cross-coupling - 4H-pyrido[1,2-a]pyrimidin-4-one - palladium - Suzuki reaction - arylation

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