Copper catalyzed halogenaton and reaction products
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United States of America Patent
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Jul 5, 2016
Grant Date -
Dec 18, 2014
app pub date -
Jun 16, 2014
filing date -
Jun 14, 2013
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Abstract
A Cu(I)-catalyzed 1,3-halogen migration reaction effectively recycles an activating group by transferring a halogen from an sp2 to a benzylic carbon with good enantioselectivity and concomitant borylation of the Ar-halo bond. The resulting enantio-enriched benzyl halide can be reacted in the same vessel under a variety of conditions to form an additional carbon-heteroatom or carbon-carbon bond while maintaining high ee. The reaction can be used to efficiently prepare novel compounds and intermediates for the preparation of therapeutics and ligands for catalysis.
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