1. Nucleophilic 18F-fluorination of phosphorofluoridates and phosphonofluoridic acids via imidazole-activated precursors.
- Author
-
Mou, Zhaobiao, Chen, Xueyuan, Wang, Chao, Wang, Tao, Yang, Hongzhang, and Li, Zijing
- Subjects
- *
POSITRON emission tomography , *IMIDAZOLES , *PHOSPHONIC acids , *PERFLUOROOCTANOIC acid , *ACIDS , *SUPERPHOSPHATES - Abstract
[Display omitted] • One-step Zn-mediated 18F-fluorination of phosphorofluoridates. • One-step Zn-mediated 18F-fluorination of phosphonofluoridic acids. • Imidazole-activated phosphates and phosphonic acids as the precursors. • High radiochemical yields, high molar activities and strong stabilities. 18F-Labeled organofluorophosphates are important radiosynthons that have only been previously accessible via 18/19F-isotope-exchange with limited molar activities. Herein, a novel 18F-fluorination methodology has been developed to prepare 18F-labeled phosphorofluoridates and phosphonofluoridic acids via the [18F]F− nucleophilic substitution of imidazole-activated precursors. The efficient one-step 18F-fluorination affords stable products in the presence of Zn(Ⅱ) with high radiochemical yields and high molar activities. This 18F-fluorination method could be used to prepare various phosphorofluoridate and phosphonofluoridic acid analogs for use as 18F-radiosynthons and potential positron emission tomography tracers. [ABSTRACT FROM AUTHOR]
- Published
- 2021
- Full Text
- View/download PDF