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An acylation‐Finkelstein approach to radioiodination of bioactives: The role of amide group anchimeric assistance

机译:一种酰化 - Finkelstein对生物灭绝的放射性碘化方法:酰胺群锚固辅助的作用

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Abstract > Herein, we report a straightforward sequential acylation‐Finkelstein approach to achieve iodination of amine containing bioactives. The utility was demonstrated by successful radiolabelling with 123 I in high radiochemical yield. Moreover, microwave‐assisted Finkelstein reaction can be employed to enhance conversion and reaction rates to obtain the desired iodides. The method is of interest for radioiodination of amine‐containing bioactives. The mechanistic details of the iodination process were studied by kinetics and density functional theory calculations, which revealed the mechanistic complexity of the reaction involving amide group anchimeric assistance. We disclose a number of fundamental aspects of amide group anchimeric assistance in substitution reactions. </abstract> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> <div class="translation abstracttxt"> <span class="zhankaihshouqi fivelineshidden" id="abstract"> <span>机译:</span><Abstract Type =“main”XML:Lang =“en”> <标题类型=“main”>摘要</标题> >在此,我们报告了一种直接的顺序酰化 - Finkelstein方法,以实现含有生物术的碘化碘化。 通过高放射化学产量的成功放射性起泡来证明该实用性。 此外,可以使用微波辅助Finkelstein反应来增强转化率和反应速率以获得所需的碘化物。 该方法对含胺的生物渗透率的放射性碘化感兴趣。 通过动力学和密度泛函理论计算研究了碘化过程的机制细节,揭示了涉及酰胺群锚固辅助的反应的机械复杂性。 我们在替代反应中披露了许多酰胺群锚固辅助的基本方面。 </ p> </ abstract> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> </div> <div class="record"> <h2 class="all_title" id="enpatent33" >著录项</h2> <ul> <li> <span class="lefttit">来源</span> <div style="width: 86%;vertical-align: text-top;display: inline-block;"> <a href='/journal-foreign-35546/'>《Journal of Physical Organic Chemistry》</a> <b style="margin: 0 2px;">|</b><span>2018年第7期</span><b style="margin: 0 2px;">|</b><span>共12页</span> </div> </li> <li> <div class="author"> <span class="lefttit">作者</span> <p id="fAuthorthree" class="threelineshidden zhankaihshouqi"> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Fjellaksel Richard&option=202" target="_blank" rel="nofollow">Fjellaksel Richard;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Dugalic Damir&option=202" target="_blank" rel="nofollow">Dugalic Damir;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Demissie Taye B.&option=202" target="_blank" rel="nofollow">Demissie Taye B.;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Riss Patrick J.&option=202" target="_blank" rel="nofollow">Riss Patrick J.;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Hjelstuen Ole‐Kristian&option=202" target="_blank" rel="nofollow">Hjelstuen Ole‐Kristian;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Sundset Rune&option=202" target="_blank" rel="nofollow">Sundset Rune;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Hansen J?rn H.&option=202" target="_blank" rel="nofollow">Hansen J?rn H.;</a> </p> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zkzz" style="display: none;">展开▼</span> </div> </li> <li> <div style="display: flex;"> <span class="lefttit">作者单位</span> <div style="position: relative;margin-left: 3px;max-width: 639px;"> <div class="threelineshidden zhankaihshouqi" id="fOrgthree"> <p>Medical Imaging Group Department of Clinical MedicineUiT The Arctic University of NorwayTroms? Norway;</p> <p>Drug Transport and Delivery Group Department of PharmacyUiT The Arctic University of NorwayTroms? Norway;</p> <p>Organic Chemistry Group Department of ChemistryUiT The Arctic University of NorwayTroms? Norway;</p> <p>Department of neuropsychiatry and psychosomatic medicineOslo University HospitalOslo Norway;</p> <p>Drug Transport and Delivery Group Department of PharmacyUiT The Arctic University of NorwayTroms? Norway;</p> <p>Medical Imaging Group Department of Clinical MedicineUiT The Arctic University of NorwayTroms? Norway;</p> <p>Organic Chemistry Group Department of ChemistryUiT The Arctic University of NorwayTroms? Norway;</p> </div> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zhdw" style="display: none;">展开▼</span> </div> </div> </li> <li > <span class="lefttit">收录信息</span> <span style="width: 86%;vertical-align: text-top;display: inline-block;"></span> </li> <li> <span class="lefttit">原文格式</span> <span>PDF</span> </li> <li> <span class="lefttit">正文语种</span> <span>eng</span> </li> <li> <span class="lefttit">中图分类</span> <span><a href="https://www.zhangqiaokeyan.com/clc/4796.html" title="有机化学一般性问题">有机化学一般性问题;</a></span> </li> <li class="antistop"> <span class="lefttit">关键词</span> <p style="width: 86%;vertical-align: text-top;"> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=amide anchimeric assistance&option=203" rel="nofollow">amide anchimeric assistance;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=bioactives&option=203" rel="nofollow">bioactives;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=DFT mechanism&option=203" rel="nofollow">DFT mechanism;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Finkelstein&option=203" rel="nofollow">Finkelstein;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=radioiodination&option=203" rel="nofollow">radioiodination;</a> </p> <div class="translation"> 机译:酰胺沉默援助;生物术;DFT机制;Finkelstein;放射碘; </div> </li> </ul> </div> </div> <div class="literature cardcommon"> <div class="similarity "> <h3 class="all_title" id="enpatent66">相似文献</h3> <div class="similaritytab clearfix"> <ul> <li class="active" >外文文献</li> <li >中文文献</li> <li >专利</li> </ul> </div> <div class="similarity_details"> <ul > <li> <div> <b>1. </b><a class="enjiyixqcontent" href="/journal-foreign-detail/0704025793864.html">An acylation‐Finkelstein approach to radioiodination of bioactives: The role of amide group anchimeric assistance</a> <b>[J]</b> . <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Fjellaksel Richard&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">Fjellaksel Richard,</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Dugalic Damir&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">Dugalic Damir,</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Demissie Taye B.&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">Demissie Taye B.,</a> <a href="/journal-foreign-35546/" target="_blank" rel="nofollow" class="tuijian_authcolor">Journal of Physical Organic Chemistry .</a> <span>2018</span><span>,第7期</span> </span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译:一种酰化 - Finkelstein对生物灭绝的放射性碘化方法:酰胺群锚固辅助的作用</span> </p> </li> <li> <div> <b>2. </b><a class="enjiyixqcontent" href="/academic-journal-foreign_journal-the-american-chemical-society_thesis/0204111714718.html">Rotating Catalysts Are Superior: Suppressing Product Inhibition by Anchimeric Assistance in Four-Component Catalytic Machinery</a> <b>[J]</b> . <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=PronayKumar Biswas&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">PronayKumar Biswas,</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Suchismita Saha&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">Suchismita Saha,</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Thomas Paululat&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">Thomas Paululat,</a> <a href="/journal-foreign-719/" target="_blank" rel="nofollow" class="tuijian_authcolor">Journal of the American Chemical Society .</a> <span>2018</span><span>,第29期</span> </span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译:旋转催化剂性能优异:四组分催化机械中的靠手性辅助抑制产物抑制</span> </p> </li> <li> <div> <b>3. </b><a class="enjiyixqcontent" href="/journal-foreign-detail/0704024112570.html">Example of a Facile Substitution of the Hydroxy Group Due to the Anchimeric Assistance of Selenium</a> <b>[J]</b> . <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Kurkutov E. 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rel="nofollow" class="tuijian_auth tuijian_authcolor">,陆洲导</a> <span> <a href="/conference-cn-59595/" target="_blank" rel="nofollow" class="tuijian_authcolor"> . 第18届全国结构工程学术会议 </a> <span> <span> . 2009</span> </span> </div> </li> <li> <div> <b>7. </b><a class="enjiyixqcontent" href="/academic-degree-domestic_mphd_thesis/020311321547.html">EGCG全酰化衍生物体外降解及对环磷酰胺引起的肝毒性的保护作用</a> <b>[A] </b> <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=杜亚俊&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor"> . 杜亚俊</a> <span> . 2016</span> </span> </div> </li> </ul> <ul style="display: none;"> <li> <div> <b>1. </b><a class="enjiyixqcontent" href="/patent-detail/06120106408948.html">放射性碘化苯甲酰胺衍生物的药用组合物及其制备方法</a> <b>[P]</b> . <span> 中国专利: CN102202503A </span> <span> . 2011-09-28</span> </div> </li> <li> <div> <b>2. </b><a class="enjiyixqcontent" href="/patent-detail/061204009203.html">聚酰胺树脂组合物、聚酰胺树脂组合物颗粒群、成型体和聚酰胺树脂组合物的制造方法</a> <b>[P]</b> . <span> 中国专利: 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