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Synthesis of astatine-tagged methylene blue, a compound for fighting micrometastases and individual cells of melanoma

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Abstract

Investigation on electrophilic attaching of astatine-211 to methylene blue is carried out. Conditions for transferring astatine to a chemically active electrophilic form were found. A method for the production of astatine-211-tagged methylene blue has been developed. The resulting radiopharmaceutical preparation is free of the nonisotopic iodine carrier. The chromatographic method of purifying simultaneously the product by anion-exchange resin QAE-Sephades A-25 allows it to pass into a 0.9% solution of sodium chloride (physiological salt solution). The method provides the radiochemical yield of astatine-211-tagged methylene blue as large as 68±6%.

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Norseev, Y.V. Synthesis of astatine-tagged methylene blue, a compound for fighting micrometastases and individual cells of melanoma. J Radioanal Nucl Chem 237, 155–158 (1998). https://doi.org/10.1007/BF02386681

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