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Synthetic Approaches to the Bifunctional Chelators for Radio­nuclides Based On Pyridine-Containing Azacrown Compounds
Synthesis ( IF 2.2 ) Pub Date : 2019-12-16 , DOI: 10.1055/s-0039-1691540
Anastasia D. Zubenko 1 , Anna A. Shchukina 1, 2 , Olga A. Fedorova 1, 2
Affiliation  

Synthetic ways to introduce functional groups (CO2Me, CO2H, OCH2CO2H, OCH2C≡CH, CH2OH, CH2Cl, CH2N3) into the pyridine ring of pyridine-containing azacrown compounds are described. These groups were introduced at position-4 of the pyridine ring, while keeping the macrocyclic carboxylate groups available for metal chelation. The derivatives were obtained by macrocyclization reaction of 4-substituted, trimethyl pyridine-2,4,6-tricarboxylate or by modification of methyl ester group in pyridine fragment of macrocycles. Obtained derivatives can be applied for preparing radiotherapeutic agents by conjugation to different vector biomolecules for targeted drug delivery to cancer cells without damaging healthy tissue.

中文翻译:

含吡啶的氮杂皇冠化合物的放射性核素双功能螯合剂的合成方法

合成的方式引进的官能团(CO 2 Me中,CO 2 H,OCH 2 CO 2 H,OCH 2 C≡CH,CH 2 OH,CH 2氯,CH 2 Ñ 3)描述了将含吡啶的氮杂冠化合物引入吡啶环中的方法。这些基团被引入吡啶环的4位,同时保持大环羧酸盐基团可用于金属螯合。所述衍生物通过4-取代的三甲基吡啶-2,4,6-三羧酸酯的大环化反应或通过修饰大环吡啶片段中的甲酯基而获得。通过与不同的载体生物分子缀合,可以将获得的衍生物用于制备放射治疗剂,以将药物靶向性递送至癌细胞而不会损害健康组织。
更新日期:2019-12-19
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