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

So Jeong Lee | Zendy; María T. Morales-Colón | Zendy; Allen F. Brooks | Zendy; Jay S. Wright | Zendy; Katarina J. Makaravage | Zendy; Peter J. H. Scott | Zendy; Melanie S. Sanford | Zendy

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S_NAr Radiofluorination with In Situ Generated [¹⁸F]Tetramethylammonium Fluoride

Author(s) -

So Jeong Lee,

María T. Morales-Colón,

Allen F. Brooks,

Jay S. Wright,

Katarina J. Makaravage,

Peter J. H. Scott,

Melanie S. Sanford

Publication year - 2021

Publication title -

the journal of organic chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.2

H-Index - 228

eISSN - 1520-6904

pISSN - 0022-3263

DOI - 10.1021/acs.joc.1c01491

Subject(s) - nucleophile , aryl , fluoride , tetramethylammonium , reagent , in situ , chemistry , combinatorial chemistry , organic chemistry , inorganic chemistry , catalysis , ion , alkyl

This report describes a method for the nucleophilic radiofluorination of (hetero)aryl chlorides, (hetero)aryl triflates, and nitroarenes using a combination of [ 18 F]KF·K 2.2.2 and Me 4 NHCO 3 for the in situ formation of a strongly nucleophilic fluorinating reagent (proposed to be [ 18 F]Me 4 NF). This method is applied to 24 substrates bearing diverse functional groups, and it generates [ 18 F](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 18 F-labeled HQ-415 for potential (pre)clinical use.

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