苄基乙醇铵离子液体和熔盐在镓和铝氟标记放射性药物合成中的应用

-Benzylethanolammonium Ionic Liquids and Molten Salts in the Synthesis of Ga- and AlF-Labeled Radiopharmaceuticals.

作者信息

Kondratenko Yulia A, Shilova Julia S, Gavrilov Vladislav A, Zolotarev Andrey A, Nadporojskii Michail A, Kochina Tatyana A, Antuganov Dmitrii O

机构信息

Grebenshchikov Institute of Silicate Chemistry RAS, Nab. Makarova, 2, 199034 Saint-Petersburg, Russia.

St. Petersburg State Technological Institute, Technical University, 26 Moskovsky Pr., 190013 Saint-Petersburg, Russia.

出版信息

Pharmaceutics. 2023 Feb 18;15(2):694. doi: 10.3390/pharmaceutics15020694.

Abstract

Ionic liquids (ILs), due to their structural features, have unique physical and chemical properties and are environmentally friendly. Every year, the number of studies devoted to the use of ILs in medicine and pharmaceutics is growing. In nuclear medicine, the use of ILs with self-buffering capacity in the synthesis of radiopharmaceuticals is extremely important. This research is devoted to obtaining new ionic buffer agents containing -benzylethanolammonium (BEA) cations and anions of carboxylic acids. A series of new BEA salts was synthesized and identified by NMR (H, C), IR spectroscopy and elemental and thermal analysis. The crystal structures of BEA hydrogen succinate, hydrogen oxalate and oxalate were determined by x-ray diffraction. Newly synthesized compounds were tested as buffer solutions in Ga- and AlF-radiolabeling reactions with a series of bifunctional chelating agents and clinically relevant peptides used for visualization of malignancies by positron emission tomography. The results obtained confirm the promise of using new buffers in the synthesis of Ga- and AlF-labeled radiopharmaceuticals.

摘要

离子液体(ILs)因其结构特点,具有独特的物理和化学性质且环境友好。每年,致力于在医学和制药领域使用离子液体的研究数量都在增加。在核医学中,具有自缓冲能力的离子液体在放射性药物合成中的应用极其重要。本研究致力于获得含有苄基乙醇铵(BEA)阳离子和羧酸阴离子的新型离子缓冲剂。通过核磁共振(H、C)、红外光谱以及元素分析和热分析合成并鉴定了一系列新型BEA盐。通过X射线衍射确定了BEA氢琥珀酸盐、氢草酸盐和草酸盐的晶体结构。将新合成的化合物作为缓冲溶液,用于与一系列双功能螯合剂以及用于正电子发射断层扫描可视化恶性肿瘤的临床相关肽进行镓和铝氟放射性标记反应。所获得的结果证实了在镓和铝氟标记放射性药物合成中使用新型缓冲剂的前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b5cd/9962170/83181990fd44/pharmaceutics-15-00694-sch001.jpg

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