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Site Selective Boron Directed <i>Ortho</i> Benzylation of <i>N</i>-Aryl Amides: Access to Structurally Diversified Dibenzoazepines
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by
Ganesh Shinde,
Hugo Castlind,
Ganesh Ghotekar,
Francoise M. Amombo Noa,
Lars Öhrström,
Henrik Sundén
Abstract
We present a highly selective protocol for the ortho benzylation of N-aryl amides. This method offers mild conditions, excellent site specificity, and scalability, enabling the synthesis of diarylmethane amides and dibenzoazepines. The protocol allows for one-pot diagonal dibenzylation of dianilides, creating valuable precursors for pharmaceutically active compounds and addressing limitations in current direct C-H activation methodologies.
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