Method for synthesis of bifunctional chelating agents-peptides
US5889146A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 26, 1997 |
| Grant date | Mar 30, 1999 |
| Priority date | — |
| Expiry date | Nov 26, 2017 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K2123/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.