55137-99-0Relevant academic research and scientific papers
Direct18F-Labeling of Biomolecules via Spontaneous Site-Specific Nucleophilic Substitution by F-on Phosphonate Prostheses
Wang, Chao,Zhang, Lei,Mou, Zhaobiao,Feng, Wanru,Li, Zhongjing,Yang, Hongzhang,Chen, Xueyuan,Lv, Shengji,Li, Zijing
supporting information, p. 4261 - 4266 (2021/05/26)
We describe a high radiochemical yield late-stage direct 18F-labeling of bare biomolecules containing common active groups. Spontaneity and site-selectivity are attributed to the remarkably higher rates of nucleophilic substitution reactions on phosphonates than on other electrophiles by F- at various hydrogen bond forms. Rapid access to many medicinally significant 18F-labeled biomolecules is achieved at 21-68% radiochemical yields and 35.9-55.1 GBq μmol-1 molar activities both manually or automatically.
Nucleophilic 18F-fluorination of phosphorofluoridates and phosphonofluoridic acids via imidazole-activated precursors
Mou, Zhaobiao,Chen, Xueyuan,Wang, Chao,Wang, Tao,Yang, Hongzhang,Li, Zijing
, (2021/03/03)
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.
