1609282-40-7Relevant academic research and scientific papers
METHODS AND COMPOSITIONS FOR DIRECT RADIOACTIVE LABELING OF BIO-ACTIVE MOLECULES AND BUILDING BLOCKS
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Paragraph 00109; 00110, (2015/11/02)
Methods of direct radioactive labeling a carbon containing compound having an sp3 C-H bond are provided. Methods of carrier-free 18F fluorination of a carbon containing compound mediated by manganese salen complexes or manganese porphyrin complexes comprising weakly coordinated anions as axial ligands are provided. Methods of "dry-down" free radioactive labeling of a carbon containing compound having an sp3 C-H bond are provided. The radioactively labeled products of the methods are provided.
Late stage benzylic C-H fluorination with [18F]fluoride for PET imaging
Huang, Xiongyi,Liu, Wei,Ren, Hong,Neelamegam, Ramesh,Hooker, Jacob M.,Groves, John T.
supporting information, p. 6842 - 6845 (2014/06/09)
We describe the first late-stage 18F labeling chemistry for aliphatic C-H bonds with no-carrier-added [18F]fluoride. The method uses Mn(salen)OTs as an F-transfer catalyst and enables the facile labeling of a variety of bioactive molecules and building blocks with radiochemical yields (RCY) ranging from 20% to 72% within 10 min without the need for preactivation of the labeling precursor. Notably, the catalyst itself can directly elute [18F]fluoride from an ion exchange cartridge with over 90% efficiency. Using this feature, the conventional and laborious dry-down step prior to reaction is circumvented, greatly simplifying the mechanics of this protocol and shortening the time for automated synthesis. Eight drug molecules, including COX, ACE, MAO, and PDE inhibitors, have been successfully [ 18F]-labeled in this way.
