Automated radiochemical synthesis of (18F)FBEM: a thiol reactive synthon for radiofluorination of peptides and proteins.

Kiesewetter DO; Jacobson O; Lang L; Chen X

首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Automated radiochemical synthesis of (18F)FBEM: a thiol reactive synthon for radiofluorination of peptides and proteins.

【24h】

Automated radiochemical synthesis of (18F)FBEM: a thiol reactive synthon for radiofluorination of peptides and proteins.

机译：（18F）FBEM的自动化放射化学合成：一种用于肽和蛋白质放射性氟化的硫醇反应性合成子。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

The automated radiochemical synthesis of N-[2-(4-[(18)F]fluorobenzamido)ethyl]maleimide ([(18)F]FBEM, IUPAC name: N-maleoylethyl-4-[(18)F]fluorobenzamide), a prosthetic group for radiolabeling the free sulfhydryl groups of peptides and proteins, is herein described. 4-[(18)F]fluorobenzoic acid was first prepared by nucleophilic displacement of a trimethylammonium moiety on a pentamethylbenzyl benzoate ester with [(18)F]fluoride. In the second step the ester was cleaved under acidic conditions. Finally, 4-[(18)F]fluorobenzoic acid was coupled to N-(2-aminoethyl)maleimide using diethylcyanophosphate and diisopropylethyl amine. Following high-performance liquid chromatography (HPLC) purification, [(18)F]FBEM was obtained in 17.3+/-7.1% yield (not decay corrected) in approximately 95 min. Isolation from the HPLC eluate and preparation for subsequent use, which was conducted manually, required an additional 10-15 min. The measured specific activity for three batches was 181.3, 251.6, and 351.5 GBq/mumol at the end of bombardment (EOB).

机译：N- [2-（4-[（[18] F]氟苯甲酰胺基）乙基]马来酰亚胺的自动放射化学合成（[（18）F] FBEM，IUPAC名称：N-马来酰基乙基-4-[（18）F]氟苯甲酰胺）本文描述了用于放射性标记肽和蛋白质的游离巯基的辅基。首先通过亲核置换五甲基苄基苯甲酸酯上的三甲基铵部分与[（18）F]氟化物，来制备4-[（（18）F]氟苯甲酸。在第二步中，将酯在酸性条件下裂解。最后，使用二乙基氰基磷酸酯和二异丙基乙基胺将4-[（（18）F]氟苯甲酸）与N-（2-氨基乙基）马来酰亚胺偶联。高效液相色谱（HPLC）纯化后，在大约95分钟内以17.3 +/- 7.1％的收率（未进行衰减校正）获得[（18）F] FBEM。从HPLC洗脱液中分离出来，并准备后续使用（手动进行）需要额外的10-15分钟。轰击（EOB）结束时，三批次的测得比活度分别为181.3、251.6和351.5 GBq / mumol。

著录项

来源
《Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine》 |2011年第2期|共5页
作者
Kiesewetter DO; Jacobson O; Lang L; Chen X;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类原子核物理学、高能物理学;
关键词

相似文献

外文文献
中文文献
专利

1. Automated radiochemical synthesis of (18F)FBEM: a thiol reactive synthon for radiofluorination of peptides and proteins. [J] . Kiesewetter DO, Jacobson O, Lang L, Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine . 2011,第2期

机译：（18F）FBEM的自动化放射化学合成：一种用于肽和蛋白质放射性氟化的硫醇反应性合成子。
2. Automated radiosynthesis of the thiol-reactive labeling agent N-(6-(4-(18F)fluorobenzylidene)aminooxyhexyl)maleimide ((18F)FBAM). [J] . Kniess T, Kuchar M, Pietzsch J Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine . 2011,第9期

机译：巯基反应性标记剂N-（6-（4-（18F）氟亚苄基）氨基氧基己基）马来酰亚胺（（18F）FBAM）的自动放射合成。
3. A thiol-reactive 18F-labeling agent, N-(2-(4-18F-fluorobenzamido)ethyl)maleimide, and synthesis of RGD peptide-based tracer for PET imaging of alpha v beta 3 integrin expression. [J] . Cai W, Zhang X, Wu Y, The Journal of Nuclear Medicine . 2006,第7期

机译：硫醇反应性18F标记剂N-（2-（4-18F-氟苯甲酰胺基）乙基）马来酰亚胺，以及基于RGD肽的示踪剂的合成，用于PET对αv beta 3整联蛋白表达的成像。
4. Synthesis of a Double Marker Synthon (NMR and Fluorescent) for Peptide Labeling [C] . Marc-Andre Bonin, Pierre Baillargeon, Martin Lepage American Peptide Symposium . 2013

机译：肽标记的双标记合成硅（NMR和荧光）的合成
5. Asymmetric synthesis of Calpha-methyl- gamma- and delta-amino acids from a common synthon and evaluation of thionyl chloride assisted peptide esterifications. [D] . Vogel, Emily Rose. 2015

机译：从常见的合成子不对称合成Calpha-甲基-γ-和δ-氨基酸，并评估亚硫酰氯辅助的肽酯化反应。
6. Automated Radiochemical Synthesis of 18FFBEM: a Thiol Reactive Synthon for Radiofluorination of Peptides and Proteins [O] . Dale O. Kiesewetter, Orit Jacobson, Lixin Lang, -1

机译：18F FBEM的自动放射化学合成：用于肽和蛋白质的酰基氟化的硫醇反应合成酮
7. Automated radiochemical synthesis of [18F]FBEM: A thiol reactive synthon for radiofluorination of peptides and proteins [O] . Dale O. Kiesewetter, Orit Jacobson, Lixin Lang, 2015

机译：自动放射化学合成[18F] FBEm：一种硫醇反应性合成子，用于肽和蛋白质的放射性氟化

Automated radiochemical synthesis of (18F)FBEM: a thiol reactive synthon for radiofluorination of peptides and proteins.

摘要

著录项

相似文献

相关主题

期刊订阅