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Updated: Aug 16, 2026

Solid Phase 11C-Methylation, Purification and Formulation for the Production of PET Tracers
Published on: October 24, 2019
Synthesis of [11C-methyl]-alpha-aminoisobutyric acid (AIB)
B Schmall1, P S Conti, M M Alauddin
1Department of Nuclear Medicine, Warren G. Magnuson Clinical Center, National Institutes of Health, Bethesda, MD 20892, USA.
Abstract:
Alpha-aminoisobutyric acid (AIB) labeled with the cyclotron-produced, positron-emitting radionuclide 11C has been synthesized with the label in the alpha-methyl group. Our previously published synthesis of [11C] AIB in the carboxyl position from [11C] HCN requires a rigorous quality assurance program to ensure that the concentration of cyanide in the final product is below certain levels. This can be avoided using the method described here with [11C] CH3I. The radiochemical yield calculated to end of bombardment (EOB) was 45-55% from [11C] CO2 with radiochemical purity of [11C-methyl] AIB exceeding 99%. Synthesis times from [11C] CO2 were about 55 min. Specific activities of 1 Ci/mumol were achieved on average. It has been shown that [11C-carboxyl] AIB is a useful imaging agent in patients with soft tissue cancers and melanoma, and it demonstrates tumor uptake in a spectrum of other animal tumor models. Because AIB is a nonmetabolized amino acid, [11C-methyl] AIB should be equally as useful. Either agent can be employed for the quantification of the A-type amino acid transport system in vivo with PET.
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