N-[(4S)-1-Methyl-2,6-Dioxohexahydropyrimidine-4-Carbonyl]-3-(Triphenylmethyl)-L-Histidyl-L-Prolineamide置于盐酸体系中,用 乙醇,水 用作溶剂,化学反应 1.0H,反应生成他替瑞林 参考文献:탈티렐린 및 이의 중간체의 신규한 제조방법 标题:탈티렐린 및 이의 중간체의 신규한 제조방법 摘要:本发明涉及一种关于新型合成塔特雷林及其中间体的制备方法,更具体地,使用fmoc(氟苯甲氧羰基)-三苄基-组氨酸作为起始原料,并通过原位反应制备塔特雷林中间体组氨酸-三苄基-脯氨酰胺,从而制备塔特雷林,相比传统技术,能够在短时间内高产率,高纯度地制备塔特雷林,适用于工业大规模生产的制备方法及其组氨酸-三苄基-脯氨酰胺的制备方法得到启示.
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
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合成参考文献
参考文献:10.1248/bpb.20.36 摘要:KINOSHITA K, FUKUSHIMA T, KODAMA Y, SUGIHARA J, YAMAMURA M, MATSUOKA Y. Chronic Anti-ataxic Actions of the Novel Thyrotropin-Releasing Hormone (TRH) Analog, TA-0910, during and after Repeated Administration in Rolling Mouse Nagoya: Behavioral and Pharmacokinetic Studies. Biological & Pharmaceutical Bulletin. 1997;20(1):36–9. doi: 10.1248/bpb.20.36. 参考文献:10.1248/bpb.20.86 摘要:KINOSHITA K, YAMAMURA M, SUGIHARA J. Distribution of Thyrotropin-Releasing Hormone (TRH) Receptors in the Brain of the Ataxic Mutant Mouse, Rolling Mouse Nagoya. Biological & Pharmaceutical Bulletin. 1997;20(1):86–7. doi: 10.1248/bpb.20.86.