METHOD FOR PRODUCING PRECURSORS FOR L-3,4-DIHYDROXY-6-[18F]FLUOROPHENYLALANINE AND 2-[18F]FLUORO-L-TYROSINE AND THE a-METHYLATED DERIVATIVES THEREOF, PRECURSOR, AND METHOD FOR PRODUCING L-3,4 DIHYDROXY-6-[18F]FLUOROPHENYLALANINE AND 2-[18F]FLUORO-L-T

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This patent describes a new and efficient method for producing chemical precursors used in the synthesis of radiolabeled amino acids, specifically L-3,4-dihydroxy-6-[18F]fluorophenylalanine ([18F]FDOPA) and 2-[18F]fluoro-L-tyrosine ([18F]FTyr), as well as their alpha-methylated derivatives. The method enables automated production with high enantiomeric purity (≥ 98%) and improved yields, making it suitable for use in automated synthesis equipment for radiotracer preparation.

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• Production of [18F]FDOPA tracers for PET imaging in Parkinson’s disease diagnosis and management.
• Production of [18F]FDOPA and [18F]FTyr for tumor diagnosis and amino acid transport studies in oncology via PET imaging.
• Automated synthesis of high-purity radiolabeled amino acids in clinical radiopharmacies and manufacturing facilities.
• Research in neurology and oncology requiring enantiomerically pure radio-labeled amino acid PET tracers.
• Development of new radiotracers for other diseases involving abnormal amino acid transport.

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• Enables automated and routine production of PET tracers with high purity, reducing the need for manual multi-step syntheses.
• Achieves high enantiomeric purity (>98%), which is crucial for accurate biological imaging and minimizing side effects or artifacts.
• Increases radiochemical yield compared to previous methods, making the process more cost-effective and efficient.
• Simplifies the synthesis process to just three radioactive steps, enhancing reproducibility and reducing potential for errors or failures.
• Compatible with commercially available automated synthesis equipment, facilitating rapid and widespread clinical adoption.
• Reduces costs associated with radiotracer production and radioisotope usage by improving efficiency and yields.
• Improvement over older electrophilic and nucleophilic synthesis methods in terms of yield, purity, automation, and scalability.

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Patent Abstract

The invention relates to a method for producing precursors for L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the a-methylated derivatives thereof, said precursor, and a method for producing L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-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 2-[18F]fluoro-L-tyrosine. The enantiomer purity of the product amounts to = 98%.