Preparing radiopharmaceuticals, useful in pharmaceutical and biochemical field e.g. diagnostic purpose, comprises producing radionuclide fluorine-18, adding precursor of radiopharmaceutical and fluorinating it by nucleophilic substitution

摘要

Preparing radiopharmaceuticals comprises: producing radionuclides fluorine-18 using heavy oxygen containing water; adding potassium carbonate; separating water; first change of the solvent to an aprotic polar solvent and adding solubilizer; adding precursor of the radiopharmaceuticals and fluorinating it by nucleophlic substitution; separating the aprotic polar solvent; second exchange of the solvent to water; cleaving the protecting groups of the precursor preferably by an acid or base catalyzed hydrolysis; and purifying the radiopharmaceuticals. Preparing radiopharmaceuticals comprises: producing radionuclides fluorine-18 ( 18F) using heavy oxygen containing water (H 218O); adding potassium carbonate; separating the water (H 218O); first solvent change to an aprotic polar solvent, preferably acetonitrile and adding a solubilizer, preferably crown ether or cryptand; adding a precursor of the radiopharmaceuticals; fluorinating the precursors by nucleophlic substitution; separating the aprotic polar solvent; second solvent change to water; cleaving the protecting groups of the precursor, preferably by an acid or base catalyzed hydrolysis; and purifying the radiopharmaceuticals. The aprotic polar solvent is less volatile than water or present in a mixture with water or a low-boiling azeotrope. The procedural steps of second solvent exchange and the cleavage of the protecting groups are carried out in a reactive distillation apparatus or reactive rectification column (19).