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Site-selective fluorination of aryl carbons in nitrogen heterocycles

A method for fluorinating aryl carbons in nitrogen heterocycles could generate new drug compounds or drug intermediates for SAR studies. In a one-step reaction at ambient temperature, the method selectively converted drug-like molecules containing pyridine, pyrazine, quinoline or other six-member nitrogen heterocycles to the corresponding 2-fluoro-substituted heterocycles at yields of 41%-99%. The method also produced a drug-like, 2-fluoropyridyl intermediate from which several 2-pyridyl-substituted compounds were generated. Future studies could include investigating whether the method can be optimized to fluorinate five-member nitrogen heterocycles.

SciBX 7(1); doi:10.1038/scibx.2014.32
Published online Jan. 9, 2014

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Fier, P.S. & Hartwig, J.F. Science; published online Nov. 22, 2013;
Contact: John F. Hartwig, University of California, Berkeley, Calif.