Carbon-11 patents (2012-2022): synthetic methodologies and novel radiotracers for PET imaging

Carbon-11 is a short-lived radionuclide with versatile applications in synthetic methodologies to develop a variety of novel PET radiotracers. Different primary and secondary carbon-11 precursors are generated from cyclotron produced [¹¹C]CO₂ and used to insert carbon-11 radionuclide into the target-specific bioactive molecules.

In this review, the patents as well as specific research articles on carbon-11 radiotracer synthesis and PET imaging applications in various diseases are mentioned since 2012 to 2022 through SciFinder database.

Carbon-11 is generally easier to insert into more organic scaffolds as a greater variety of functional groups. Despite the short half-life of carbon-11 radionuclide (t_1/2 = 20.4 min), it is widely used in PET radiotracer development due to its direct insertion into bioactive compounds and less isotopic dilution unlike other positron emitters like fluorine-18. Various synthons can be easily generated using the primary and secondary carbon-11 precursors . The carbon-11 radiotracers provide target-oriented information associated with the pharmacology, and physiological conditions of the disease status. Various protocols and automated methods were adapted for easy and convenient synthesis of carbon-11 radiotracers. The PET advances drug development and clinical trials by revealing biological target engagement, proof of mechanism, pharmacokinetic, and pharmacodynamic profiles of new drug candidates using selective radiotracers.