Published January 1, 2012 | Version v1
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Catalyst- and Base-Controlled Site-Selective sp2 and sp3 Direct Arylation of 5,7-Dimethyl-2-phenylpyrazolo[1,5-a]pyrimidine Using Aryl Bromides

  • 1. Univ Orleans, CNRS, UMR 7311, Inst Chim Organ & Analyt, F-45067 Orleans 2, France
  • 2. Univ Victor Segalen Bordeaux 2, EA4318 Pharmacochim, UFR Sci Pharmaceut, F-33076 Bordeaux, France

Description

The palladium-catalyzed direct CH arylation of various heterocyclic is now recognized to be the most effective methodology for making aromatic compounds. In this paper, we present a new approach to control the site-selective direct CH arylation of both sp2 and sp3 sites in 5,7-dimethyl-2-phenylpyrazolo[1,5-a]pyrimidine by using aryl bromides. The desired compounds were obtained in satisfactory yields. The effects of each reaction parameter including catalyst, base, and solvent were investigated.

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