Process for the production of radioiodinated neuroreceptor agents

摘要

The present invention is related to process for producing radioiodinate neuroreceptor agents with improves yields. In said process the trialkyltin group of the precursor of the neuroreceptor agent is replaced by radioiodine in the presence of an oxidation agent, preferably chloramine T in a pH adjusted by a buffering system comprising inorganic or organic acids and their salts. The end-products are subsequently separated from the by-products using chromatographic separation methods such as high performance liquid chromatography (HPLC), wherein the mobile solvent phase comprises a mixture of ethanol and water having a pH of 1-6. The improved yield are obtainable by preventing the formation of volatile radioactive by-products and by using a non-toxic solvent system in the chromatographic separation process, which simplifies the down stream processing of the end product.