N-[2-(叔丁氧羰基氨基)乙基]甘氨酸乙酯盐酸盐置于盐酸体系中,用 乙醚 作为反应溶剂,化学反应 1.17H,以77%的收率获得产物n-(Boc-氨基乙基)甘氨酸乙酯盐酸盐 参考文献:Pharmaceuticals For Enhanced Delivery To Disease Targets 标题:Pharmaceuticals For Enhanced Delivery To Disease Targets 摘要:用于增强治疗疾病靶向性的药物包括一对化合物.第一化合物包括第一寡肽与第一基团共轭,用于与诊断或治疗活性剂偶联.第二化合物包括第二寡肽与靶向物种共轭,该靶向物种具有能够结合目标的靶向基团.第二寡肽具有与第一寡肽互补的序列.第一和第二寡肽可以是互补的pna序列.这些药物通过方法被注入到患者体内,用于诊断或治疗疾病状态,或评估疾病状态治疗的有效性.
专利号:WO-2004037772-A1 优先权日:2002-10-22 标 题 :Convenient and scalable synthesis of ethyl n-[(2-boc-amino) ethyl] glycinate and its hydrochloride salt 发明人:HUDSON ROBERT H E; VIIRRE RUSSELL D 权利人:UNIV WESTERN ONTARIO; HUDSON ROBERT H E; VIIRRE RUSSELL D 摘要:The present invention discloses an improved synthesis of ethyl N-[(2-Boc-amino)ethyl]glycinate and its hydrochloride salt. The synthesis is based on the reductive alkylation of Boc-ethylenediamine with ethyl glyoxylate hydrate and furnishes the title compound in near quantitative yield and high purity without chromatography. This compound is suitable, as is, for the synthesis peptide nucleic acid monomers. Further, conversion to the hydrochloride salt provides a stable, non-hygroscopic solid that is a convenient form for handling and storage.
专利号:AU-2003278025-A1 优先权日:2002-10-22 标 题 :Convenient and scalable synthesis of ethyl n-((2-boc-amino) ethyl) glycinate and its hydrochloride salt
专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/s12039-020-1738-y 摘要:Das A, Pradhan B. A facile route to synthesize N-(Boc-Aminoethylglycin)thymine Ethyl Ester, application to the synthesis of PNA-oligonucleotide conjugates. Journal of Chemical Sciences. 2020 Jan 29;132(1):32. doi: 10.1007/s12039-020-1738-y.