Stoichiometry-focused 18F-labeling of alkyne-substituted oligodeoxynucleotides using azido([18F]fluoromethyl)benzenes by Cu-catalyzed Huisgen reaction
Stoichiometry-focused 18F-labeling of alkyne-substituted oligodeoxynucleotides using azido([18F]fluoromethyl)benzenes by Cu-catalyzed Huisgen reaction
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DOI：
10.1016/j.bmc.2010.11.033
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发表时间：
2011-01-01
影响因子：
3.5
通讯作者：
Doi, Hisashi
中科院分区：
文献类型：
--
作者：
Kuboyama, Takeshi;Nakahara, Motoi;Doi, Hisashi
通过Cu催化的Huisgen反应，开发了一种用于F-18-放射性标记寡脱氧核苷酸（ODNs）的新方法，该方法使用尽可能低的量的前体生物分子，用于实现化学计量导向的PET（正电子发射断层扫描）化学。在优化的环化反应条件下，在CuSO 4、TBTA [三氟甲基]苯和炔取代的ODN（20 nmol）存在下，在40 ℃下反应15 min（（1-苄基-1H-1，2，3-三唑-4-基）甲基）胺]和抗坏血酸钠（2：1：2）、合成具有足够高的放射性（2.1- 2.5GBq）和比放射性（1800-2400 GBq/g）的F-18标记的ODN，已经完成了用于动物和人类PET研究的μ mol。(C)2010爱思唯尔有限公司版权所有。
A novel method for F-18-radiolabeling of oligodeoxynucleotides (ODNs) by a Cu-catalyzed Huisgen reaction has been developed by using the lowest possible amount of the precursor biomolecule for the realization of stoichiometry-oriented PET (positron emission tomography) chemistry. Under the optimized cyclization conditions of p- or m-azido([F-18]fluoromethyl)benzene and alkyne-substituted ODN (20 nmol) at 40 degrees C for 15 min in the presence of CuSO4, TBTA [tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl) amine], and sodium ascorbate (2:1:2), the synthesis of F-18-labeled ODNs with sufficiently high radioactivities of 2.1-2.5 GBq and specific radioactivities of 1800-2400 GBq/mu mol have been accomplished for use in animal and human PET studies. (C) 2010 Elsevier Ltd. All rights reserved.