Literature DB >> 34505779

SNAr Radiofluorination with In Situ Generated [18F]Tetramethylammonium Fluoride.

So Jeong Lee1,2, María T Morales-Colón3, Allen F Brooks1, Jay S Wright1, Katarina J Makaravage3, Peter J H Scott1, Melanie S Sanford3.   

Abstract

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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Year:  2021        PMID： 34505779      PMCID： PMC8826450          DOI： 10.1021/acs.joc.1c01491

Source DB:  PubMed          Journal:  J Org Chem        ISSN： 0022-3263            Impact factor:   4.198


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Journal:  Nat Protoc       Date:  2020-04-08       Impact factor: 13.491

7.  Anhydrous Tetramethylammonium Fluoride for Room-Temperature S(N)Ar Fluorination.

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