化学
亲核细胞
芳基
四甲基铵
试剂
原位
氟化物
组合化学
有机化学
无机化学
催化作用
离子
烷基
作者
So Jeong Lee,María T Morales-Colón,Allen F. Brooks,Jay Wright,Katarina J. Makaravage,Peter J. H. Scott,Melanie S. Sanford
标识
DOI:10.1021/acs.joc.1c01491
摘要
This report describes a method for the nucleophilic radiofluorination of (hetero)aryl chlorides, (hetero)aryl triflates, and nitroarenes using a combination of [18F]KF·K2.2.2 and Me4NHCO3 for the in situ formation of a strongly nucleophilic fluorinating reagent (proposed to be [18F]Me4NF). This method is applied to 24 substrates bearing diverse functional groups, and it generates [18F](hetero)aryl fluoride products in good to excellent radiochemical yields in the presence of ambient air/moisture. The reaction is applied to the preparation of 18F-labeled HQ-415 for potential (pre)clinical use.
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