CAS: 78664-73-0; Posatirelin

📜(S)-2-哌啶酮-6-羧基 酸置于三乙胺,N,N'-二环己基碳二亚胺体系中,用 乙酸乙酯,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 5.0H,反应生成 泊替瑞林
参考文献:促甲状腺激素释放激素类似物的合成.2.具有高度中枢神经系统活性的三肽结构上不同于trh.
标题:促甲状腺激素释放激素类似物的合成.2.具有高度中枢神经系统活性的三肽结构上不同于trh.
摘要:通过五氟苯基酯法合成了一系列新的促甲状腺激素释放激素(trh)类似物,这些类似物是通过进一步修饰我们最有效的中枢神经系统(cns)在两个末端刺激中性三肽而获得的,并测试了cns和促甲状腺激素(tsh)释放活动.[leu2]中的吡咯-2-氨基己二酸,2-氧代咪唑烷-4-羧酸或γ-丁内酯-γ-羧酸取代脯氨酸谷氨酸,脯氨酸由哌啶酸,噻唑烷-4-羧酸或高脯氨酸代替脯氨酸.-和[nva2] Trh导致三肽结构上与trh大不相同.尽管如此,17种类似物中的7种(1,2,8-10,16和17)比trh具有更强的抗感性作用,激素作用微乎其微或无.当焦谷氨酸在n端被焦-2-氨基己二酸取代时,Cns活性最高[paad-Leu-Pro-Nh2,1(rgh 2202)和paad-Nva-Pro-Nh2,2].还描述了适用于大规模制备的l-2-氨基己二酸的新颖合成.
DOI:10.1021/jm00159A015

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: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-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.

专利号:US-2022372022-A1
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics

专利号:US-10919882-B2
优先权日:2019-05-09
标题:Compounds for use in synthesis of peptidomimetics