METHOD OF PRODUCING A UREA DERIVATIVE WITH A CHELATE CENTRE, TROPIC TO A PROSTATE-SPECIFIC MEMBRANE ANTIGEN FOR BINDING TECHNETIUM-99M / RHENIUM FOR DIAGNOSING / TREATING PROSTATE CANCER Russian patent published in 2019 - IPC C07D401/12 C07C275/24 A61K51/04 A61K103/10 

FIELD: technological processes.

SUBSTANCE: invention relates to a method of producing a urea derivative with a chelate centre, tropic to a prostate-specific membrane antigen for binding technetium-99m/rhenium 188/186 for diagnosing prostate cancer. Method involves obtaining a conjugate of a prostate-specific membrane antigen (PSMA) inhibitor with a succinimide ester chelating agent ω-bis(pyridin-2-ylmethyl)amino)aliphatic acids. Inhibitor of PSMA used is (3S,7S,25S,28S)-33-amino-25,28-dibenzyl-5,13,20,23,26,29-hexaoxo-4,6,12,29,24,27,30-heptaazatrioctane-1,3,7-tricarboxylic acid. Chelating agent used is succinimid-1-yl 6-(bis(pyridin-2-ylmethyl)amino)hexanoate. Chelating agent is added to the inhibitor in molar ratio 1:1.2–5.0 in 10–200 mmol of phosphate, or borate, or carbonate buffer with pH 6.5–9.0, or in purified water, or in physiologic saline of sodium chloride with addition and/or without acetonitrile or dimethylformamide, synthesis is carried out at room temperature for 2–12 hours while stirring or incubated for 12–24 hours at temperature 5–10 °C, then the product is purified by semi-preparative high-performance chromatography.

EFFECT: disclosed method enables to obtain an end product with high output, which can be used for diagnosing prostate cancer.

1 cl, 21 ex, 9 dwg