A Transmetalation Reaction Enables the Synthesis of [18F]5-Fluorouracil from [18F]Fluoride for Human PET Imaging was written by Hoover, Andrew J.;Lazari, Mark;Ren, Hong;Narayanam, Maruthi Kumar;Murphy, Jennifer M.;van Dam, R. Michael;Hooker, Jacob M.;Ritter, Tobias. And the article was included in Organometallics in 2016.Name: Benzo[b]thiophen-3-ylboronic acid This article mentions the following:
Translation of new 18F-fluorination reactions to produce radiotracers for human positron emission tomog. (PET) imaging is rare because the chem. must useful scope and the process for 18F-labeled tracer production must be robust and simple to execute. The application of transition metal mediators has enabled impactful 18F-fluorination methods, but to date none of these reactions were applied to produce a human-injectable PET tracer. The authors present chem. and process innovations that culminate in the 1st production from [18F]fluoride of human doses of [18F]5-fluorouracil, a PET tracer for cancer imaging in humans. The 1st preparation of Ni σ-aryl complexes by transmetalation from arylboronic acids or esters was developed, and enabled the synthesis of the [18F]5-fluorouracil precursor. Routine production of >10 mCi doses of [18F]5-fluorouracil was accomplished with a new instrument for azeotrope-free [18F]fluoride concentration in a process that leverages the tolerance of H2O in Ni-mediated 18F-fluorination. In the experiment, the researchers used many compounds, for example, Benzo[b]thiophen-3-ylboronic acid (cas: 113893-08-6Name: Benzo[b]thiophen-3-ylboronic acid).
Benzo[b]thiophen-3-ylboronic acid (cas: 113893-08-6) belongs to benzothiophene derivatives. Benzothiophenes are valuable heterocycles that are widely used in medicines, agrochemicals, and materials science. It is found within the chemical structures of pharmaceutical drugs such as zileuton, raloxifene, and sertaconazole, and also BTCP.Name: Benzo[b]thiophen-3-ylboronic acid
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem