CycloSiFA: The Next Generation of Silicon-Based Fluoride Acceptors for Positron Emission Tomography (PET).
Angew Chem Int Ed Engl
; 62(50): e202309002, 2023 Dec 11.
Article
em En
| MEDLINE
| ID: mdl-37850849
ABSTRACT
The ring-opening Si-fluorination of a variety of azasilole derivatives cyclo-1-(iPr2 Si)-4-X-C6 H3 -2-CH2 NR (4 R=2,6-iPr2 C6 H3 , X=H; 4 a R=2,4,6-Me3 C6 H2 , X=H; 9 R=2,6-iPr2 C6 H3 , X=tBuMe2 SiO; 10 R=2,6-iPr2 C6 H3 , X=OH; 13 R=2,6-iPr2 C6 H3 , X=HCCCH2 O; 22 R=2,6-iPr2 C6 H3 , X=tBuMe2 SiCH2 O) with different 19 F-fluoride sources was studied, optimized and the experience gained was used in a translational approach to create a straightforward 18 F-labelling protocol for the azasilole derivatives [18 F]6 and [18 F]14. The latter constitutes a potential clickable CycloSiFA prosthetic group which might be used in PET tracer development using Cu-catalysed triazole formation. Based on our findings, CycloSiFA has the potential to become a new entry into non-canonical labelling methodologies for radioactive PET tracer development.
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Bases de dados:
MEDLINE
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Ano de publicação:
2023
Tipo de documento:
Article
País de afiliação:
Alemanha