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通过微波增强环加成反应轻松获得用于医学成像应用的异双金属配合物。

Easy access to heterobimetallic complexes for medical imaging applications via microwave-enhanced cycloaddition.

作者信息

Desbois Nicolas, Pacquelet Sandrine, Dubois Adrien, Michelin Clément, Gros Claude P

机构信息

Université de Bourgogne Franche-Comté, ICMUB (UMR CNRS 6302), 9 Avenue Alain Savary, BP 47870, 21078 Dijon Cedex, France.

出版信息

Beilstein J Org Chem. 2015 Nov 17;11:2202-8. doi: 10.3762/bjoc.11.239. eCollection 2015.

Abstract

The Cu(I)-catalysed Huisgen cycloaddition, known as "click" reaction, has been applied to the synthesis of a range of triazole-linked porphyrin/corrole to DOTA/NOTA derivatives. Microwave irradiation significantly accelerates the reaction. The synthesis of heterobimetallic complexes was easily achieved in up to 60% isolated yield. Heterobimetallic complexes were easily prepared as potential MRI/PET (SPECT) bimodal contrast agents incorporating one metal (Mn, Gd) for the enhancement of contrast for MRI applications and one "cold" metal (Cu, Ga, In) for future radionuclear imaging applications. Preliminary relaxivity measurements showed that the reported complexes are promising contrast agents (CA) in MRI.

摘要

铜(I)催化的惠斯根环加成反应,即“点击”反应,已应用于一系列三唑连接的卟啉/咕啉到DOTA/NOTA衍生物的合成。微波辐射显著加速了该反应。异双金属配合物的合成很容易实现,分离产率高达60%。异双金属配合物很容易制备成潜在的MRI/PET(SPECT)双模态造影剂,其中包含一种用于增强MRI应用对比度的金属(锰、钆)和一种用于未来放射性核素成像应用的“冷”金属(铜、镓、铟)。初步弛豫率测量表明,所报道的配合物在MRI中是有前景的造影剂(CA)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af87/4660971/54c3ef01a7da/Beilstein_J_Org_Chem-11-2202-g002.jpg

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