9H-Fluoren-9-Ylmethyl (4R)-4-Methyl-5-Oxo-1,3-Oxazolidine-3-Carboxylate置于三乙基硅烷,三氟乙酸体系中,用 氯仿 用作溶剂,化学反应 16.0H,以23.8 G的收率获得n-芴甲氧羰酰基-N-甲基-D-丙氨酸 参考文献:Total Synthesis Of (+)-Azinothricin And (+)-Kettapeptin 标题:Total Synthesis Of (+)-Azinothricin And (+)-Kettapeptin 摘要:Asymmetric Total Syntheses Of (+)-Azinothricin And (+)-Kettapeptin Have Been Completed Through A Common New Pathway That Exploits A Highly Chemoselective Coupling Reaction Between The Fully Elaborated Cyclodepsipeptide 5 And The Glycal Activated Esters 3 And 4 At The Final Stages Of Both Respective Syntheses. Doi:10.1021/ol802817T
专利号:CN-104284891-A 优先权日:2012-03-17 标 题:Conformational Restricted Total Synthesis of Macrocyclic Compounds
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.