1207429-53-5Relevant academic research and scientific papers
Synthesis of 18F-Labeled Aryl Fluorosulfates via Nucleophilic Radiofluorination
Kwon, Young-Do,Jeon, Min Ho,Park, Nam Kyu,Seo, Jeong Kon,Son, Jeongmin,Ryu, Young Hoon,Hong, Sung You,Chun, Joong-Hyun
, p. 5511 - 5516 (2020)
Sulfuryl fluoride gas is a key reagent for SO2F transfer. However, conventional SO2F transfer reactions have limited 18F-radiochemistry translation, due to the inaccessibility of gaseous [18F]SO2F2. Herein, we report the first SO2F2-free synthesis of aryl [18F]fluorosulfates from both phenolic and isolated aryl imidazylate precursors with cyclotron-produced 18F-. The radiochemical yields ranged from moderate to good with excellent functional group tolerance. The reliability of our approach was validated by the automated radiosynthesis of 4-acetamidophenyl [18F]fluorosulfate.
O-(Aminosulfonylation) of phenols and an example of slow hydrolytic release
Yang, Baocheng,Sun, Zhexun,Liu, Changzhi,Cui, Yan,Guo, Zhilei,Ren, Yuwei,Lu, Zhijian,Knapp, Spencer
supporting information, p. 6658 - 6661 (2014/12/11)
Sequential replacement of imidazole from sulfonyldiimidazole by phenols and then amines leads to O-arylsulfamate esters. Application of this coupling method to 19 phenols and 6 amines generates a library of 114 sulfamate esters, Ar-OSO2-NR2. A sulfamate based conjugate of ethinyl estradiol was prepared by using the steroid 3-hydroxyl as the phenol component, and an amino amide derived from linoleic acid as the amine. Hydrolysis of this conjugate was studied in aqueous buffer at pH values 2, 5, and 7.4, and (essentially identical) respective half-lives of 6.8, 6.6, and 6.7 days were observed.
