Journal
TETRAHEDRON LETTERS
Volume 51, Issue 14, Pages 1906-1909Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2010.02.042
Keywords
Fluorodenitration; Microwave; F-18; PET; Haloperidol; Donepezil; Nitrodehalogenation
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Funding
- Alzheimer's Drug Discovery Foundation (ADDF)
- Institute for the Study of Aging (ISOA) Inc [281004]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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