Tetrahedron Letters

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

M Jamous, U Haberkorn, W Mier

Index: Jamous, Mazen; Haberkorn, Uwe; Mier, Walter Tetrahedron Letters, 2012 , vol. 53, # 50 p. 6810 - 6814

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Citation Number: 4

Abstract

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 ...