![]() ![]() The first procedure details the synthesis of an 18F–synthon and its subsequent ligation to the cysteine residue of Arg–Gly–Asp–Cys in 10.5 h from commercially available starting materials (189-min radiosynthesis). To expand the utility of nucleophilic aromatic substitution with fluorine-18, we describe two complementary procedures for the radiodeoxyfluorination of bench-stable and easy-to-access phenols that ensure rapid access to densely functionalized electron-rich and electron-poor 18F–aryl fluorides. Peptide substrates, which are highly desirable targets for PET molecular imaging, are particularly challenging to label with fluorine-18 because they are densely functionalized and sensitive to high temperatures and basic conditions. ![]() Furthermore, many protic functional groups are incompatible with basic fluoride anions. Nucleophilic aromatic substitution is the most widely employed reaction to functionalize aromatic substrates with the radioactive fluorine-18 but its scope is restricted to arenes containing electron-withdrawing substituents. The challenge of forming C– 18F bonds is often a bottleneck in the development of new 18F-labeled tracer molecules for noninvasive functional imaging studies using positron emission tomography (PET).
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