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

P LaBeaume, M Placzek, M Daniels, I Kendrick, P Ng…

Index: LaBeaume, Paul; Placzek, Michael; Daniels, Mathew; Kendrick, Ian; Ng, Patrick; McNeel, Melissa; Afroze, Roushan; Alexander, Abigail; Thomas, Rhiannon; Kallmerten, Amy E.; Jones, Graham B. Tetrahedron Letters, 2010 , vol. 51, # 14 p. 1906 - 1909

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Citation Number: 23

Abstract

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 10min, rendering it practical for use in the preparation of F18 labeled ligands for PET imaging. Application of the method in the synthesis of CNS agents is demonstrated, and a practical ...