CAS: 204318-14-9; 2,2',2''-(10-(2-(((R)-1-(((4R,7S,10S,13R,16S,19R)-13-((1H-Indol-3-yl)Methyl)-10-(4-Aminobutyl)-4-(((2R,3R)-1,3-Dihydroxybutan-2-yl)Carbamoyl)-16-(4-Hydroxybenzyl)-7-((R)-1-Hydroxyethyl)-6,9,12,15,18-Pentaoxo-1,2-Dithia-5,8,11,14,17-Pentaazacycloicosan-19-yl)Amino)-1-Oxo-3-Phenylpropan-2-yl)Amino)-2-Oxoethyl)-1,4,7,10-Tetraazacyclododecane-1,4,7-Triyl)Triacetic Acid

上下游产品

Tyr3-Octreotide 103667-46-5

📜在 一水合肼体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 0.17H,反应生成依多曲肽
参考文献:使用未保护的dota快速高产地液相合成dota-Tyr 3-奥曲肽和dota-Tyr 3-奥曲肽
标题:使用未保护的dota快速高产地液相合成dota-Tyr 3-奥曲肽和dota-Tyr 3-奥曲肽
摘要:用大环螯合剂dota(1)对tyr 3-Lys 5(dde)-奥曲肽(toc(dde))和tyr 3-Lys 5(dde)-奥曲肽(tate(dde))进行溶液相衍生化的改进方法1,4,7,10-四氮杂ñ ',ñ ",ñ ''',ñ ⁗n'-四乙酸)已被开发.完全保护的亲本肽是使用fmoc策略通过固相肽合成(spps)组装的.从固体载体上裂解后,使用h 2 O 2进行二硫键的形成..在水/ Dmf溶剂系统中,在nhs,Edci和dipea存在下,Toc(dde)和tate(dde)均成功与dota偶联.偶联反应的收率仅在2小时内> 98%,且未检测到副产物的形成.因此,该制备dotat°C,Dotatate和其他dota-肽缀合物的方法是当前使用的方法的快速且经济的替代方法.
Doi:10.1016/s0040-4039(03)00221-1

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

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-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:US-2023382819-A1
优先权日:2020-10-14
标 题:Processes for synthesis of alpha-emitting radiopharmaceuticals
发明人：MORSE DAVID L; WADAS THADDEUS J; PANDYA DARPAN; TAFRESHI NARGES; BUDZEVICH MIKALAI
权利人:H LEE MOFFITT CANCER CT & RES; UNIV IOWA RES FOUND
摘要:The present disclosure provides processes for the preparation of alpha emitting radiopharmaceutical compositions, in particular DOTATATE complexes of alpha emitting radionuclides, as well as use of such prepared compositions in the treatment of cancers.

专利号:US-11440881-B2
优先权日:2019-05-09
标题 :Thiosemicarbazates and uses thereof
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.