DOTA-tris(OPp ester) as a bifunctional prochelator for the preparation of DOTA-peptide conjugates
Peptides containing the chelator DOTA have gained importance for molecular imaging and therapy with radionuclides. However, all synthons described for the convergent solid phase synthesis of DOTA-peptide conjugates show windows of stability that are too narrow to allow a clean and convergent deprote...
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| Main Authors: | , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
10 October 2012
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| In: |
Tetrahedron letters
Year: 2012, Volume: 53, Issue: 50, Pages: 6810-6814 |
| ISSN: | 1873-3581 |
| DOI: | 10.1016/j.tetlet.2012.10.007 |
| Online Access: | Verlag, Volltext: http://dx.doi.org/10.1016/j.tetlet.2012.10.007 Verlag, Volltext: http://www.sciencedirect.com/science/article/pii/S0040403912017558 
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| Author Notes: | Mazen Jamous, Uwe Haberkorn, Walter Mier |
| Summary: | Peptides containing the chelator DOTA have gained importance for molecular imaging and therapy with radionuclides. However, all synthons described for the convergent solid phase synthesis of DOTA-peptide conjugates show windows of stability that are too narrow to allow a clean and convergent deprotection process. The synthesis of the new prochelator DOTA-tris(OPp ester) starting from cyclen is reported. Using this prochelator for the synthesis of several DOTA peptide conjugates revealed that its cleavage—in contrast to the cleavage of DOTA-tris(tBu ester) conjugates—does not require an extended deprotection time, and therefore results in clean and homogenous products. |
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| Item Description: | Available online 10 October 2012 Gesehen am 10.07.2018 |
| Physical Description: | Online Resource |
| ISSN: | 1873-3581 |
| DOI: | 10.1016/j.tetlet.2012.10.007 |