39740-30-2Relevant articles and documents
NOVEL HIGH PENETRATION DRUGS AND COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON'S DISEASE
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Paragraph 0098-0100, (2020/04/24)
PROBLEM TO BE SOLVED: To provide novel high penetration compositions (HPCs) or high penetration prodrugs (HPPs) for treatment of Parkinson's disease. SOLUTION: The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after c
Convenient synthesis of diaryliodonium salts for the production of [18F]F-DOPA
Edwards, Richard,Westwell, Andrew D.,Daniels, Stephen,Wirth, Thomas
supporting information, p. 625 - 630 (2015/01/30)
[18F]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 [18F]F-DOPA through reaction with no carrier added (n.c.a.) nucleophilic [18F]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 [18F]F-DOPA.
Fluorination of an arylboronic ester using [18F]selectfluor bis(triflate): Application to 6-[18F]fluoro-l-DOPA
Stenhagen, Ida S. R.,Kirjavainen, Anna K.,Forsback, Sarita J.,Jorgensen, Charlotte G.,Robins, Edward G.,Luthra, Sajinder K.,Solin, Olof,Gouverneur, Veronique
supporting information, p. 1386 - 1388 (2013/02/25)
The Ag-mediated electrophilic [18F]fluorination of an arylboronic ester is reported. This new radiochemical transformation uses [ 18F]selectfluor bis(triflate) in acetone. The process gave 6-[ 18F]fluoro-l-DOPA with a RCY of 19 ± 12% and a specific activity of 2.6 ± 0.3 GBq μmol-1.