This article reports an efficient CH activation process for regioselective halogenation of 1,4-benzodiazepinones. Direct halogenation with NXS (X = Br, I) affords halogenated benzodiazepinones on the central aromatic ring whereas catalyst (Pd(OAc)2) controlled CH activation furnishes regioselectively ortho halogenated benzodiazepinones on the phenyl side chain.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4503988 | PMC |
| http://dx.doi.org/10.1038/srep12131 | DOI Listing |
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