Author/Authors :
Wنngler، نويسنده , , Bjِrn and Beck، نويسنده , , Carmen and Wagner-Utermann، نويسنده , , Ulrike and Schirrmacher، نويسنده , , Esther and Bauer، نويسنده , , Claudia and Rِsch، نويسنده , , Frank and Schirrmacher، نويسنده , , Ralf and Eisenhut، نويسنده , , Michael، نويسنده ,
Abstract :
The synthesis of tris-allyl-DOTA starting from cyclen and its application in the preparation of DOTA–peptide conjugates is reported. Clinically important conjugates such as DOTA–Tyr3-octreotide (DOTA–TOC), DOTA–Tyr3-octreotate (DOTA–TATE) as well as a DOTA–RGD peptide were synthesized in high yields with Fmoc solid phase peptide synthesis. The final, extremely reliable de-allylation was achieved on solid phase by different methods identifying morpholine/Pd(0) as the most suitable one obtaining all DOTA peptide conjugates in high yields. All DOTA–peptides were purified by reversed phase HPLC and structural identity was proved using MALDI-TOF mass spectrometry.
