Molecular Renovation Strategy for Expeditious Synthesis of Molecular Probes

Molecular probes are useful chemical tools that are widely applied in life science research, including in molecular biology and drug discovery. However, the preparation of molecular probes often requires considerable time and effort even if the synthesis is conducted by well-trained organic chemists. This is mostly due to the complex structure of the target molecules or their precursors, which typically contain sensitive functional moieties. Furthermore, the synthetic route to probes must frequently be modified from that of the original compounds because the functional moiety of the probe should be preferably introduced into the molecule at a late stage of the synthesis. To address these issues, we propose a new concept that we named a molecular renovation strategy that can expedite the synthesis of molecular probes. This approach involves direct transformation of the original bioactive compounds to the probe precursors, followed by the introduction of a functional moiety. This account describes our recent efforts to realize this concept, particularly made for expeditious preparation of imaging probes for positron emission tomography (PET) via transition metal-catalyzed borylation reactions via cleavage of stable chemical bonds and transition metal-mediated deborylative radiolabeling reactions with PET nuclides.