Institute of Nuclear Energy Research

Kung-Tsung Wang

Shui-Tein Chen

Lie-Hang Shen

Te-Wei Lee

Shyh-Yi Chyi

Zei-Tsan Tsai

Shiang-Rong Chang

Gann Ting

Tian-Fu Huang

Chang-Mau Shing

This invention is a novel synthesis of BCA-peptides (BCA: bifunctional chelating agents). In this method, the starting material--Fmoc-Thr(ol)-Terephthal-Acetal-Amide Resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)-Terephtha l-Acetal-Amide Resin was obtained. This compound reacted with iodine to give disulfide-containing peptide resin of ##STR1## Cleavage of the peptide from the resin was achieved by TFA. The cleavaged peptide was protected by the reaction of octreotide with di-t-butyldicarbonate. BCA was coupled to the selectively protected octreotide. This product was obtained by reaction of protected BCA-peptides with TFA. The final product was labeled by radioisotope .sup.111 InCl.sub.3 for tumor imaging radiopharmaceuticals.

Method for synthesis of bifunctional chelating agents-peptides

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Taipei, Taiwan

Kung-Tsung Wang