选择氟
化学
试剂
卤化
氯化物
组合化学
表面改性
氯
有机化学
物理化学
作者
Susanne Gradl,Viviane Zantop,Peter Gmeiner,Harald Hübner,Markus R. Heinrich
出处
期刊:ChemMedChem
[Wiley]
日期:2023-05-08
卷期号:18 (15)
被引量:1
标识
DOI:10.1002/cmdc.202300144
摘要
Abstract By using active pharmaceutical ingredients (APIs) previously recovered from expired drugs, it is shown that Selectfluor can act as a reagent for operationally simple late‐stage fluorination and chlorination of electron‐rich arenes under mild reaction conditions. As shown in mechanistic experiments, aromatic fluorination thereby competes with chlorine‐for‐fluorine exchange on Selectfluor and subsequent aromatic chlorination, whereat the chloride ions may either be provided by the hydrochloride salt of the respective API or by triethylammonium chloride. Biological testing of the fluorinated or chlorinated APIs at adrenergic, dopaminergic, muscarinergic, opioid or serotoninergic receptors demonstrated that improved binding affinities can be achieved via this straightforward strategy.
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