Comparison and systematic optimization of synthetic protocols for DOTA-hydrazide generation

TETRAHEDRON LETTERS

卷:54

Article

Fuge, Felix¹  Weiler, Marek¹  Gaetjens, Jessica¹  Lammers, Twan^1,2,3  Kiessling, Fabian¹ 

[1] Rhein Westfal TH Aachen, Helmholtz Inst Biomed Engn, Dept Expt Mol Imaging, D-52074 Aachen, Germany

[2] Univ Twente, MIRA Inst Biomed Technol & Tech Med, Dept Targeted Therapeut, NL-7500 AE Enschede, Netherlands

[3] Univ Utrecht, UIPS, Dept Pharmaceut, NL-3584 CG Utrecht, Netherlands

关键词: Cyclen;    Alkylation;    Hydrazide;    DOTA;    Lanthanides;   

DOI  :  10.1016/j.tetlet.2012.11.151

来源: Elsevier

【 摘 要 】

DOTA-based organometallic complexes are extensively used in functional and molecular imaging studies, as well as in radioimmunotherapy. DOTA forms thermodynamically stable and kinetically inert complexes with various different diagnostic and therapeutic metals, such as gadolinium, gallium, yttrium and indium. Here, we have compared and systematically optimized the two most commonly used synthetic protocols for generating DOTA-hydrazide complexes, identifying conditions which reduce overall reaction time and increase overall yield (C) 2012 Elsevier Ltd. All rights reserved.

【 授权许可】

Free