Application of tris-allyl-DOTA in the preparation of DOTA-peptide conjugates |
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Authors: | Björn Wängler Carmen Beck Esther Schirrmacher Frank Rösch Michael Eisenhut |
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Institution: | a German Cancer Research Center, Department of Radiopharmaceutical Chemistry, D-69120 Heidelberg, Germany b University of Mainz, Department of Nuclear Medicine, D-55126 Mainz, Germany c University of Mainz, Institute of Nuclear Chemistry, D-55128 Mainz, Germany |
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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. |
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