发明名称 Polymer precursors of radiolabeled compounds, and methods of making and using the same
摘要 One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.
申请公布号 US9023317(B2) 申请公布日期 2015.05.05
申请号 US201313776039 申请日期 2013.02.25
申请人 University of Western Ontario 发明人 Hunter Duncan H.;Janabi Mustafa
分类号 A61K51/00;A61M36/14;C08G18/48;C07B59/00;A61K51/06;C07K1/04;C08F8/32;C08F8/42;C07C231/14;C07D207/06;C07D211/14;C07D295/13 主分类号 A61K51/00
代理机构 K&L Gates LLP 代理人 K&L Gates LLP ;Vito Christine C.;Wu Pei
主权项 1. A method of synthesizing a radiolabeled benzamide on a solid support comprising: a) selecting a solid support comprising at least one compound attached to said solid support, wherein the compound is selected from the group consisting of: Poly-(4S,5S)-2-(5-{dibutyl[2-(4-vinylphenyl)ethyl]stannyl}-2,3-dihydrobenzofuran-7-yl)-3,4-dimethyl-5-phenyl-1,3-oxazolidine-co-divinylbenzene;Poly-(4S,5S)-2-(4-{dibutyl[2-(3-vinylphenyl)ethyl]stannyl}phenyl)-3,4-dimethyl-5-phenyl-1,3-oxazolidine-co-divinylbenzene; andPoly-(4S,5S)-2-(4-{dibutyl[2-(4-vinylphenyl)ethyl]stannyl}phenyl)-3,4-dimethyl-5-phenyl-1,3-oxazolidine-co-divinylbenzene; b) reacting said compound with at least one acid to afford a benzoic acid moiety or a carboxylic acid moiety; c) reacting said moiety of said compound attached to said solid support with at least one amine to afford a benzamide bound to a solid support; and d) reacting said benzamide bound to said solid support with a radioisotope; and an oxidant selected from the group consisting of chloramine-T,N-chlorosuccinimide, tert-butylhydroperoxide, iodogen, iodobeads and meta-chloroperbenzoic acid; to yield said radiolabeled benzamide.
地址 London, Ontario CA