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Updated: Jun 23, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Modular synthesis of cyclic β-difluoroamines
Natalie G Charlesworth1, Dhanarajan Arunprasath1, Mark A Graham2
1School of Chemistry, GlaxoSmithKline Carbon Neutral Laboratories for Sustainable Chemistry, University of Nottingham, 6 Triumph Road, Nottingham NG7 2GA, UK. ross.denton@nottingham.ac.uk.
Abstract:
Fluorine-containing saturated nitrogen heterocycles are very attractive structures in medicinal and biological chemistry because fluorine can be used to tune conformation as well as key properties such as basicity and bioavailability. At present cyclic fluorinated amines are accessed using hazardous reagents such as DAST or by lengthy synthesis routes. Here we report a modular two-step synthesis of cyclic β-fluoroalkyl amines using a photoredox-catalysed cyclisation/hydrogen atom transfer reaction of bromodifluoroethylamines.
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