Synthesis and Derivatization of 1,1-[18 F]Difluorinated Alkenes.
Angew Chem Int Ed Engl
; 58(2): 472-476, 2019 01 08.
Article
in En
| MEDLINE
| ID: mdl-30452114
ABSTRACT
A general method for the synthesis of 1,1-[18 F]difluorinated alkenes from [18 F]fluoride is reported. This transformation is highly regioselective giving the desired 18 F-fluoroalkenes with radiochemical purities of up to 77 % within 20 minutes and a molar activity (Am ) of 1â
GBq µmol-1 . The transformations are operationally simple to perform and were readily translated onto a commercial automated synthesis unit. The resultant 1,1-[18 F]difluorinated alkene motif is prevalent in numerous drug molecules, and this is the first general method to synthesize this motif with fluorine-18. 18 F-fluorinated alkenes are excellent building blocks and participate in a number of post-labeling transformations to access a range of 18 F-perfluorinated functional groups that have never before been radiolabeled with non-carrier-added [18 F]fluoride. This method considerably expands the range of 18 F-motifs accessible to radiochemists.
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01-internacional
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MEDLINE
Language:
En
Journal:
Angew Chem Int Ed Engl
Year:
2019
Document type:
Article
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