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Approach to PET cancer screening : developments of low molecule probe tagged gallium-68 and carbon-11labeling method

PET癌症筛查方法：镓68标记低分子探针和碳11标记方法的发展

基本信息

批准号：
20790027
负责人：
YOSHIOKA Eito
金额：
$ 2.66万
依托单位：
Hyogo University of Health Sciences
依托单位国家：
日本
项目类别：
Grant-in-Aid for Young Scientists (B)
财政年份：
2008
资助国家：
日本
起止时间：
2008 至 2010
项目状态：
已结题

项目摘要

I paid attention to the positron-emitting radionuclide, especially gallium-68 and carbon-11, and developed the following reactions using an unstable chemical species such as aryne and radical for the label based on high-speed reactions. In addition, I developed the oxidation-reduction reaction using the photocatalyst for capture of CO_2.First, to develop gallium-68 probe, I studied aryne based Huisgen-type reaction under the metal-free condition and desired benztriazole was obtained in excellent yield. I also reported the [2+2] type reaction, insertion of aryne into the C=O π-bond of formamides, and the subsequent trapping process of the benzoxetene intermediate with dialkylzincs. In addition, under mild condition, I reported the multi-component coupling reaction leading chromenes, coumarins and xanthenes via the insertion into π-bond of DMF. Moreover, I reported the cascade addition-cyclization-trapping reaction involving the unfavorable mismatched interaction of nucleophilic radicals, together with the control of enantioselectivities. And I reported the results of experiments to prove the utility of the polycrystalline TiO_2 (P25) in the hydrogenation of aromatic ketones.

我注意到了正电子放射性核素，特别是镓-68和碳-11，并开发了以下反应，使用不稳定的化学物种，如芳炔和自由基的标记基于高速反应。此外，还开发了利用该光催化剂捕获CO_2的氧化还原反应。首先，为了开发Ga-68探针，在无金属条件下，研究了芳炔基的Huisgen型反应，以优异的产率得到了苯并三唑。还报道了芳炔插入甲酰胺C=O π键的[2+2]型反应，以及随后的苯并氧杂环丁烯中间体与二烷基锌的捕获过程。此外，在温和条件下，还报道了苯并吡喃、香豆素和氧杂蒽通过插入DMF的π-键进行的多组分偶联反应。此外，我报道了级联加成-环化-捕获反应，涉及亲核自由基的不利错配相互作用，以及对映选择性的控制。并报道了多晶TiO_2（P25）在芳香酮加氢反应中的应用实验结果。