DOTA-tris(OPp ester) as a bifunctional prochelator for the preparation of DOTA-peptide conjugates

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• 作者：Mazen Jamous ; Uwe Haberkorn ; Walter Mier ; ^{walter.mier@med.uni-heidelberg.de}
• 关键词：Radiopeptides ; Bifunctional chelating agents ; DOTA-based prochelator ; Protecting group
• 刊名：Tetrahedron Letters
• 出版年：2012
• 出版时间：12 December, 2012
• 年：2012
• 卷：53
• 期：50
• 页码：6810-6814
• 全文大小：605 K

文摘

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¡ªin contrast to the cleavage of DOTA-tris(tBu ester) conjugates¡ªdoes not require an extended deprotection time, and therefore results in clean and homogenous products.