Journal of the American Chemical Society
Page 4 of 5
Ed. 2016, 53, 11543. (d) Salman, M.; Zhu, Z.-Q.; Huang, Z.-Z. Org. Lett. 2016,
In conclusion, we have developed a practical Cu(II)-catalyzed
ortho-selective aminomethylation of free phenols that provides
access to Csp2–Csp3 coupling products under mild conditions. This
transformation was found to be high selective for functionalizing
the position ortho to the hydroxyl group. A variety of functional
groups were tolerated, and good to excellent yields were afforded.
We also demonstrated a convenient synthesis of biologically ac-
tive molecules with this method. Highly selective functionaliza-
tion of free phenols has rarely been reported. Thus, we anticipate
that this method will be highly useful, particularly in light of its
simplicity and broad scope.
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Supporting Information
Experimental procedures and spectral data for new compounds
(14) For Ru catalysis, see: (a) Ye, Y.; Sanford, M. S. J. Am. Chem. Soc.
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Tellis, J. C.; Molander, G. A. Proc. Natl. Acad. Sci. 2015, 112, 12026. (f) Tellis,
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AUTHOR INFORMATION
Corresponding Author
*dhwang@sioc.ac.cn
Notes
The authors declare no competing financial interests.
ACKNOWLEDGMENT
We gratefully acknowledge support from the National Key R&D
Program of China (2016YFA0202900), the Strategic Priority
Research Program of the Chinese Academy of Sciences
(XDB20000000), and the "Thousand Recruitment Program for
Young Professionals".
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