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 prepa
Microwave accelerated three-component fluoroalkylations: expeditious routes to fluoropharmaceuticals and PET ligands
β Scribed by Michael Placzek; Paul LaBeaume; Luke Harris; Patrick Ng; Mathew Daniels; Amy Kallmerten; Graham B. Jones
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- French
- Weight
- 496 KB
- Volume
- 52
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
One-pot three-component coupling methods have been developed to allow in situ preparation of fluoroalkylated arenes and hydrocarbon chain analogs. The methods, which are accelerated under microwave irradiation gives access to x-fluorinated alkyl, alkenyl, and alkynyl substituted arenes from readily available precursors. The methods involve late stage introduction of the fluorine and are well suited to application in the synthesis of 18 F labeled PET imaging agents.
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