Site Selective\nBoron Directed <i>Ortho</i> Benzylation of <i>N</i>‑Aryl Amides: Access to\nStructurally Diversified Dibenzoazepines

We present a highly selective protocol for the <i>ortho</i> benzylation of <i>N</i>-aryl amides. This\nmethod offers\nmild conditions, excellent site specificity, and scalability, enabling\nthe synthesis of diarylmethane amides and dibenzoazepines. The protocol\nallows for one-pot diagonal dibenzylation of dianilides, creating\nvaluable precursors for pharmaceutically active compounds and addressing\nlimitations in current direct C–H activation methodologies.

Publication Details

Journal
Figshare
Published
2024-12-17
DOI
https://doi.org/10.1021/acs.orglett.4c04196.s001
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Site Selective\nBoron Directed Ortho Benzylation of N‑Aryl Amides: Access to\nStructurally Diversified Dibenzoazepines

Figshare
Catalytic C–H Functionalization Methods
article

Site Selective\nBoron Directed Ortho Benzylation of N‑Aryl Amides: Access to\nStructurally Diversified Dibenzoazepines

article en

Abstract

We present a highly selective protocol for the <i>ortho</i> benzylation of <i>N</i>-aryl amides. This\nmethod offers\nmild conditions, excellent site specificity, and scalability, enabling\nthe synthesis of diarylmethane amides and dibenzoazepines. The protocol\nallows for one-pot diagonal dibenzylation of dianilides, creating\nvaluable precursors for pharmaceutically active compounds and addressing\nlimitations in current direct C–H activation methodologies.

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Openalex Percentile: Top 72%
Catalytic C–H Functionalization Methods
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