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Synfacts 2010(7): 0848-0848  
DOI: 10.1055/s-0029-1220094
Polymer-Supported Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

Solid-Phase Synthesis of Pyrimidines, Pyrazoles, and Isoxazoles

Contributor(s): Yasuhiro Uozumi, Yoichi M. A. Yamada, Chung Keun Jin
G. Pellegrino, F. Leonetti*, A. Carotti, O. Nicolotti, L. Pisani, A. Stefanachi, M. Catto
University of Bari, Italy
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Publication History

Publication Date:
22 June 2010 (online)

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Significance

A solid-phase synthesis of pyrimi­dines, pyrazoles, and isoxazoles was described. Thus, resin-supported enamino ketone derivatives III were prepared from an Fmoc-protected Rink amide resin in three steps. The cyclization of III with guanidines was carried out in the presence of the phosphazene base BEMP under microwave ­irradiation to afford the corresponding pyrimidine derivatives 1-18 in 69-73% yield.