A modular Rh-catalyzed entry to azepines is outlined. Under a CO atmosphere, protecting group directed C-C bond activation of aminocyclopropanes provides rhodacyclopentanones. These intermediates are effective for intramolecular C-H metalation of either an N-aryl or N-vinyl unit en route to azepine ring systems. Thus, byproduct-free heterocyclizations are enabled by sequential C-C activation and C-H functionalization steps.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5834216 | PMC |
| http://dx.doi.org/10.1021/jacs.7b13087 | DOI Listing |
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