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Article Abstract
Herein, we develop a metal-free, nondirected, site-selective, one-pot approach to -arylation of arylamines. This Brønsted acid-catalyzed, direct C-C bond formation offers a broad substrate scope and scalability and creates the ideal conditions for overriding the conventional site-selectivity to furnish -substituted anilines. Additionally, the protocol applies to the -allylation of anilines and has been extended to afford late-stage functionalization and synthesis of medicinally privileged arylated diamines and densely functionalized anilines. The control experiments and density functional theory studies provide evidence for the proposed mechanism and selectivity.
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| http://dx.doi.org/10.1021/acs.orglett.3c02181 | DOI Listing |
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