CAS: 294-90-6; 1,4,7,10-Tetraazacyclododecane

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2-溴乙胺置于二碳酸二叔丁酯体系中,用 甲醇 用作溶剂,化学反应 24.0H,反应生成轮环藤宁
参考文献:询问受体介导的机制的作用:肽功能化的放射性标记的金纳米粒子在肿瘤小鼠中的生物学命运.
标题:询问受体介导的机制的作用:肽功能化的放射性标记的金纳米粒子在肿瘤小鼠中的生物学命运.
摘要:为了更好地了解肽缀合的纳米颗粒向肿瘤的转运机制,我们进行了在人前列腺癌荷瘤小鼠体内由蛙皮素(bbn)肽功能化的金纳米颗粒(aunps)的体内生物学研究.最初,我们试图将aunp与dtpa和dota类型的无环和大环螯合剂的硫醇衍生物进行比较.Dtpa衍生物无法提供67Ga的稳定配位,因此,仅对含dota的aunp进行了bbn类似物的功能化.用bbn [7-14]使用不明的胱氨酸基团或双齿的硫代基团将附着dota的金纳米颗粒官能化,以连接肽段.硫代组的使用导致aunps表现出最高的体外细胞内在化作用(约25%,15分钟),大大提高.然而,这些结果不能转化为体内肿瘤吸收.在荷瘤小鼠中静脉内(iv)和腹膜内(ip)施用纳米缀合物后的生物分布研究表明,Bbn的存在在一定程度上影响了纳米构建体的生物学特性.对于静脉内给药,Epr效应似乎抵消了受体介导的途径.相比之下,在ip给药中,有理由认为grpr介
Doi:10.1021/acs.Bioconjchem.6B00102

专利信息

专利号:US-10189803-B2
优先权日:2008-02-22
标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions
发明人：CHONG HYUN-SOON
权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH
摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

专利号:US-2024082435-A1
优先权日:2021-02-26
标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents
发明人：PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS
权利人:TELIX INT INNOVATIONS PTY LTD
摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.

专利号:WO-2023148680-A1
优先权日:2022-02-04
标 题 :Methods for large scale synthesis of radionuclide complexes
发明人：BARBATO DONATO; BO MICHELE; ROSSETTO MATTIA; TEDESCO MATTIA; VALERIO FEDERICO
权利人:ADVANCED ACCELERATOR APPLICATIONS
摘要:The present disclosure relates to methods of large scale synthesis of radionuclide complex solutions having a high activity for diagnostic and/or therapeutic purposes, their use in the commercial production of radioactive drug substances, and to respective solutions as well as containers comprising said solutions.

专利号:US-7851621-B2
优先权日:2005-06-30
标 题:Synthesis of deoxybiotinyl hexamethylenediamine-dota
发明人：MARZI MAURO; DI MARZO MARIA
权利人:SIGMA TAU IND FARMACEUTI
摘要:A process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as a base.

专利号:US-9447149-B2
优先权日:2012-03-06
标 题 :Methods and compositions for the rapid synthesis of radiometal-labeled probes
发明人：CHEN KAI; CONTI PETER STEPHEN
权利人:UNIV SOUTHERN CALIFORNIA
摘要:The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.

专利号:US-9988388-B2
优先权日:2012-11-21
标 题:Synthesis of imidazo[1,2-a]pyrazin-4-ium salts for the synthesis of 1,4,7-triazacyclononane (tacn) and N- and/or C- functionalized derivatives thereof
发明人：DENAT FRANCK; DESOGERE PAULINE; BERNHARD CLAIRE; ROUSSELIN YOANN; BOSCHETTI FREDERIC
权利人:UNIV BOURGOGNE; CENTRE NAT RECH SCIENT
摘要:A compound with formula (V′) n nthe synthesis method for compound (V′), and its use for the preparation of 1,4,7-triazacyclononane (tacn) and N- and/or C-functionalized derivatives thereof, particularly compounds with formula (I)n n nAlso, metallic complexes comprising a ligand with formula (I) and a metal and their use for imaging.