Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation

Hajer Abdelkafi (1) , Jean-Christophe Cintrat (1)

1 SCBM - Service de Chimie Bio-Organique et de Marquage

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.

Domains: Life Sciences [q-bio]

Hajer Abdelkafi, Jean-Christophe Cintrat. Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation. Scientific Reports, 2015, 5 (1), ⟨10.1038/srep12131⟩. ⟨cea-02075732⟩