发明名称 Use of aniline in the radiostabilization of oxime ligation
摘要 The disclosure relates to the use of aniline or a salt or derivative thereof selected from the group consisting of 4-methoxyaniline, 4-nitroaniline, 2,6-dimethylaniline, a deuterated aniline derivative or a polymer-bound aniline, as a radiostabilizer in a method comprising the step of reacting a radiolabeled aldehyde (I) with an aminooxy (II) in the presence of aniline (III) to form imine-oxy (IV) (abstract figure). The method is performed at a pH of about 1.0-7.0, and the starting activity of the radiolabeled aldehyde (I) is at least 50 GBq. The radiolabelled aldehyde may further contain a radiolabelled organic or biological moiety, such as alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclyl, heteroaryl, cycloalkyl, amino acid, peptide, or vector moieties. The radiolabel may be radioisotope suitable for PET or SPECT imaging. The aminooxy may further contain any organic or biological moiety. The disclosure also relates to the use of aniline as a radiostabilizer in a method comprising the step of reacting a aldehyde with a radiolabeled aminooxy to form an imine-oxy.
申请公布号 NZ612151(A) 申请公布日期 2015.08.28
申请号 NZ20110612151 申请日期 2011.12.15
申请人 GE HEALTHCARE LIMITED 发明人 ENGELL TORGRIM;OSBORN NIGEL
分类号 A61K47/48;A61K51/04;A61K51/08;C07C47/00;C07C211/46;C07C249/04;C07C251/34 主分类号 A61K47/48
代理机构 代理人
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