CAS: 60239-18-1; 2,2',2'',2'''-(1,4,7,10-Tetraazacyclododecane-1,4,7,10-Tetrayl)Tetraacetic Acid

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1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸四叔丁酯置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 16.0H,以85%的收率获得产物1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸
参考文献:直接测量气相配位配合物水合状态的一般方法:变温质谱法
标题:直接测量气相配位配合物水合状态的一般方法:变温质谱法
摘要:基于金属的诊断和治疗的三元水复合物的形成与其体内功效密切相关,但量化配位水配体存在的方法是有限的.我们介绍了一种通用的高通量方法,用于基于变温离子阱串联质谱法表征气相中顺磁性和反磁性配位配合物的水合状态.三元水复合物可直接在质谱中观测到,并作为离子阱温度的函数进行量化.我们恢复了镧系元素水合的预期周期性趋势,并通过检查温度相关的物种形成曲线来区分具有几种内球水配体的配合物.我们推导出可辨别的内球和第二球水合事件的气相热力学参数,并讨论它们在预测溶液相行为方面的应用.水在内部和外部球体中结合的温度差异主要来自熵效应.这种方法的广泛适用性使我们能够在活跃的临床前和临床研究中估计 Ga,Sc 和 Zr 配合物的水合状态,但水合数尚未确定.变温质谱仪作为表征和量化元素周期表内球体水合作用趋势的通用工具而出现.sc 和 Zr 配合物正在进行积极的临床前和临床研究,水合值尚未确定.变温质谱仪作为表征和
DOI:10.1021/jacs.9B05874

专利信息

专利号:US-9446995-B2
优先权日:2012-05-21
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 INST 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-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-2013267680-A1
优先权日:2010-09-15
标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof
发明人：OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL
权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST
摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.

专利号:US-6451543-B1
优先权日:1998-08-31
标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides
发明人：KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO
权利人:GRYPHON SCIENCES
摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.

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:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.