Squaric Acid Bisphposphonates for Theranostics of Bone Metastasis - the Easy DOTA-Zoledronate.

Lukas Greifenstein, Nils Engelbogen, Domokos Máthé, Tilmann Grus, Frank Rösch, Ralf Bergmann
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Abstract

Bisphosponates are an interesting molecular class and in recent years their application has found its way into radiopharmaceutical research and thus into molecular imaging. In addition to great imaging of bone metastases, bisphospnate-based tracers for imaging also have some significant drawbacks. For example, their synthesis is often difficult. Additionally, this can lead to complex and almost impossible purification and quality control. This has limited the production and labeling of suitable molecular and their widespread use to a few facilities. Our squaric acid-based approach provides a way to overcome these problems and makes the synthesis as well as the purification of the compounds much easier. In addition, we were able to demonstrate that labeling with 68Ga is possible under the typical conditions.

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用于骨转移治疗的方酸双膦酸盐——简单的DOTA唑来膦酸盐
双磷酸盐是一个有趣的分子类别,近年来,它们的应用已进入放射性药物研究,从而进入分子成像。除了对骨转移瘤进行良好的成像外,用于成像的双磷酸盐示踪剂也有一些显著的缺点。例如,它们的合成通常很困难。此外,这可能导致复杂且几乎不可能的纯化和质量控制。这限制了合适分子的生产和标记及其在少数设施中的广泛使用。我们基于方酸的方法提供了一种克服这些问题的方法,并使化合物的合成和纯化更加容易。此外,我们能够证明在典型条件下用68Ga标记是可能的。
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