Ten new N-(2-benzimidazolylmethyl)iminodiacetic acids (BIMIDA)* have been synthesized from the corresponding o-phenylenediamines via intermediate 2-chloromethyl and 2-aminomethyl benzimid- azoles as ligands for 99mTc. Anomalies associated with the synthesis of the iodo-substituted compound are described.

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summaryTo exploit the tissue affinity of compounds for radiopharmaceutical purposes, attachment of chelating groups is usually necessary to facilitate technetium-99m binding and transport.The chelating group, iminodiacetic acid, previously used to modify lidocaine for hepatobiliary radiopharmaceuticals, was attached to several antibiotic sulfanilamides known to concentrate in certain transplanted animal tumors.These iminodiacetic acid derivatives were labelled with technetium-9% by the stannous chloride reduction method.Biodistribution of the ' % T c labelled compounds in tumor bearing rats revealed no specific concentration in the tumors and localization mainly in the excretory organs.The results indicate that, as in the case of lidocaine, conversion of the sulfanilamides into imindiacetic acid derivatives and chelation with technetium leads to an altered biodistribution and loss of biological specificity.

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