Here, reported is a new method for divergent synthesis of functionalized tetrahydroquinolines (THQs), featuring a biomedically interesting azabicyclo[4.1.0]heptane core, proceeding with mild conditions, good substrate and functionality tolerance, and operational simplicity. Mechanistic studies suggest that the products are formed via carbonucleophilic 1,4-addition-induced dearomatization of quinolinium salts and intramolecular cyclopropanation with α-halo ketones followed by α-nucleophilic addition with different nucleophiles. The present work lays a foundation to access new N-heterocycles via the dearomative tandem functionalization of azaarenes.
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| http://dx.doi.org/10.1021/acs.joc.4c00783 | DOI Listing |
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