Abstract

AbstractChloroquine can be iodinated with radioactive iodine in radiochemical yields 60‐75% with chloramine‐T or H2O2/lactoperoxidase. With both methods a rather complex mixture of labelled products is formed. The yield and ratios of the labelled products depend upon the chloroquine‐concentration, the amount of carrier iodide present and in the case of the chloramine‐T method, the chloramine‐T concentration. With the chloramine‐T method the main product is 3‐iodochloroquine, with H2O2/lactoperoxidase an unidentified iodinated chloroquine‐derivative, probably a dimer, is the main labelled product. With chloramine‐T products such as 3‐chlorochloroquine and deethylchloroquine are formed in mass amounts.

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