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Microwave-accelerated fluorodenitrations and nitrodehalogenations: expeditious routes to labeled PET ligands and fluoropharmaceuticals

✍ Scribed by Paul LaBeaume; Michael Placzek; Mathew Daniels; Ian Kendrick; Patrick Ng; Melissa McNeel; Roushan Afroze; Abigail Alexander; Rhiannon Thomas; Amy E. Kallmerten; Graham B. Jones

Publisher: Elsevier Science
Year: 2010
Tongue: French
Weight: 345 KB
Volume: 51
Category: Article
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2010.02.042

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✦ Synopsis

Methods for the expeditious fluorination of arenes have been investigated, using readily available fluoride sources. An optimized procedure for microwave-accelerated fluorodenitration has been developed, giving good to excellent yields in less than 10 min, rendering it practical for use in the preparation of F 18 labeled ligands for PET imaging. Application of the method in the synthesis of CNS agents is demonstrated, and a practical method for the preparation of substrates is also presented.

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