Convenient Synthesis of Diaryliodonium Salts for the Production of [18F]F‐DOPA. Issue 3 (9th December 2014)

• Record Type: Journal Article
• Authors: Edwards, Richard; Westwell, Andrew D.; Daniels, Stephen; Wirth, Thomas
• Is Part Of: European journal of organic chemistry. Issue 3(2015)
• Page Start: 625
• Page End: 630
• Publication Date: 2014-12-09
• Subjects: Analytical methods -- Isotopic ­labeling -- Imaging agents -- Fluorination -- PET -- Radiochemistry; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1002/ejoc.201403378
• Languages: English
• ISSNs: 1434-193X

Abstract

Abstract: [ 18 F]F‐DOPA is an important radiotracer that is used in the diagnosis of Parkinson's disease and neuroendocrine tumours. We describe a simple synthesis for a number of diaryliodonium salt precursors that are suitable for the production of [ 18 F]F‐DOPA through reaction with no carrier added (n.c.a.) nucleophilic [ 18 F]fluoride. The simple procedure gives bench‐stable, complex iodonium precursors in good yields without the need for laborious anhydrous conditions. Further alteration to the precursor counterion can be readily achieved for a range of halides and pseudo halides by a simple modification of the workup. Preliminary "hot" and "cold" fluorination results show the suitability of the compounds for the production of [ 18 F]F‐DOPA. Abstract : A simple protocol has been developed leading to bench‐stable, complex iodonium precursors for the synthesis of [ 18 F]F‐DOPA.