ArticleACS medicinal chemistry letters2025
General Synthesis and Properties of Bridged, Fused, and Spirocyclic Azacycles via Intramolecular C-H Bond Amination.
Article in ACS medicinal chemistry letters, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Rational Design and Structure-Activity Relationship Analysis of Decalin-Based High-Energy-Density Fuel Molecules.Molecules (Basel, Switzerland) · 2026Article
- Strain Release of 1-Azabicyclo[1.1.0]butanes as a Gateway to Highly Functionalized Azetidines: New Strategies and Structural Motifs.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Review
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9 authors.
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Abstract
General methods to construct complex azacycles significantly enable the invention of new therapeutics. Herein, we describe a unified strategy to access bridged, fused, and spirocyclic bicyclic azacycles leveraging a Hofmann-Löffler-Freytag (HLF) approach. Our method yields value-added and complexity-enriched amines through an intramolecular C-H bond functionalization, converting monocyclic amines to bicyclic amines in a single step. Depending on the connectivity between the amine and the monocyclic ring, we are able to access bridged, fused, and spirocyclic architectures. Additionally, the physicochemical properties of these bicyclic amines were evaluated, and it was found that bridged amines tend to be less lipophilic in comparison to their monocyclic matched pairs.
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