A General 11C-Labeling Approach Enabled by Fluoride-Mediated Desilylation of Organosilanes

Wenhao Qu presents a general 11C-labeling strategy using a fluoride-mediated desilylation (FMDS) process

Positron emission tomography (PET) is an important imaging modality for the non-invasive investigation of biochemical and molecular events in living organisms. Because of the ubiquitous presence of carbon atoms in organic molecules, 11C-labeled organic compounds with well-characterized biological and pharmacological properties could be used for clinical and pre-clinical studies with much fewer hurdles, compared with compounds labeled with other radioisotopes (such as 18F, 123I and 76Br). In addition, the short half-life of 11C allows the performance of multiple studies on the same subject in a single site visit, which represents a great advantage in clinical studies. To produce the desired 11C-labeled compounds in high radiochemical and chemical purities, as well as with high molecular activity, there is a still unmet demand to develop fast and reliable approaches for introducing 11C into molecules with diversified structures. Recently, Professor Wenhao Qu at Stony Brook University (USA) and his colleagues reported a general 11C-labeling strategy using a fluoride-mediated desilylation (FMDS) process to generate reactive nucleophiles for nucleophilic 11C-carboxylation and 11C-methylation.

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