High-Yielding Automated Convergent Synthesis of No-Carrier-Added [C-11-Carbonyl]-Labeled Amino Acids Using the Strecker Reaction

摘要

A new variant of the Strecker synthesis using no-carrier-added [C-11] cyanide for the synthesis of radiolabeled amino acids is described. The protocol is fully automated using a radiochemistry synthesis module and applied to the production of a number of new PET radiotracers. [C-11-Carbonyl] sarcosine, [C-11-carbonyl] methionine, [C-11-carbonyl]- N-phenylglycine, and [C-11-carbonyl] glycine are all synthesized in moderate to good radiochemical yields. The synthesis of [C-11-carbonyl] sarcosine has been validated for production of doses for clinical use, and preliminary evaluation of the new radiotracer in PC3 tumor-bearing mice is also reported.