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Synfacts 2008(11): 1205-1205  
DOI: 10.1055/s-0028-1083462
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

C-OH Bond Activation and Arylation of Tautomerizable Heterocycles

Contributor(s): Paul Knochel, Tobias Thaler
F.-A. Kang*, Z. Sui, W. V. Murray
Johnson & Johnson Pharmaceutical Research and Development, Exton, USA
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Publication History

Publication Date:
23 October 2008 (online)

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Significance

Direct arylation via C-OH bond activation of enolizable heterocycles with aryl boronic acids using PyBroP is reported. The reaction tolerates various functionalities, among them very sensitive functional groups, such as nitro and ester groups. Using this method, 6-arylpurine ribonucleosides can be prepared in only one step, as no protection of the OH groups on the sugar is required.