Site Selective Boron Directed Ortho Benzylation of N-Aryl Amides: Access to Structurally Diversified Dibenzoazepines

Journal article, 2025

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.