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Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation.


ABSTRACT: 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.

SUBMITTER: Abdelkafi H 

PROVIDER: S-EPMC4503988 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature

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Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation.

Abdelkafi Hajer H   Cintrat Jean-Christophe JC  

Scientific reports 20150716


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. ...[more]

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