Preparation of Radiopharmaceuticals through Arylthallium Ditrifluoroacetate Intermediate

Arylthallium ditrifluoroacetate를 중간체(中間體)로 하는 방사성의약품(放射性醫藥品)의 합성법(合成法)

Amino acids such as L-tyrosine, L-histidine, and tryptophan, which bear an aromatic ring in the molecule, could successfully be labelled by radioactive iodine through arylthallium ditrifluoroacetate intermediate. Generally, the labelling reaction could proceed in a short labelling time(ca, 20 minutes) and resulted in a high labelling yields and purity of the labelled product. This procedure has, therefore, been proved to be effective as the labelling method of short labelling time and high specific activity. Labelling proteins such as oval albumin and human albumin could also be achieved in $34\sim48%$ net labelling yield by thallating them at the low temperature $(0\sim10^{\circ}C)$, whereas the labelled products were mainly composed of various denatured products by thallating them at the high temperature$(35\sim40^{\circ}C)$, though the radioactivity was highly retained in the labelled products. Uracil and hippuric acid could also be labelled in a short labelling time though their thallation required a prolonged heating procedure. It was proved that this procedure may be effective to label these compounds by short lived radioisotopes. The labelling yields were, however, lower than 30%.