METHOD FOR PRODUCING PRECURSORS FOR L-2-[18F]FLUOROPHENYLALANINE AND 6-[18F]FLUORO-L--META-TYROSINE AND THE a-METHYLATED DERIVATIVES THEREOF, PRECURSOR, AND METHOD FOR PRODUCING L-2-[18F]FLUOROPHENYLALANINE AND 6-[18F]FLUORO-L-META-TYROSINE AND THE a

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This patent describes a method for producing high-purity radiolabeled amino acids, specifically L-2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine, including their alpha-methylated derivatives. The invention includes new chemical precursor compounds and an efficient, automatable synthesis process that achieves very high enantiomeric purity (≥98%). The method is suitable for use in automated equipment commonly found in radiopharmaceutical production facilities.

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• Production of radiolabeled amino acids for use as PET (Positron Emission Tomography) imaging tracers, particularly in oncology and neurology.
• Supply chain for hospitals and imaging centers to obtain clinical-grade, high-purity PET tracers.
• Research applications where enantiomerically pure radiolabeled amino acids are needed to study metabolic pathways or disease mechanisms.
• Automated synthesis modules in radiopharmaceutical facilities for routine, safe, and efficient production of PET tracers.

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• Provides a synthesis process yielding radiolabeled amino acids with exceptionally high enantiomeric purity (≥98%), improving diagnostic accuracy.
• Compatible with automated synthesis equipment, reducing manual handling and enhancing safety, especially important for radioactive compounds.
• Uses fewer synthetic steps and achieves higher radiochemical yields, lowering production costs and waste.
• Reduces the risk of contamination and racemization, ensuring product consistency and suitability for clinical and research applications.
• Enables reliable, routine production of PET tracers, supporting consistent supply for medical imaging.

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Patent Abstract

The invention relates to a method for producing precursors for L-2-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine and the a-methylated derivatives thereof, said precursor, and a method for producing L-2-[18F]fluorophenylalanine and 2-[18F]fluoro-L-meta-tyrosine and the a-methylated derivatives thereof from the precursor. According to the invention, a compound of formula (3) is used to enable an automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 6-[18F]fluoro-L-meta-tyrosine. The enantiomer purity of the product amounts to = 98%.