Total Synthesis of Rapamycin

Steven V. Ley; Miles N. Tackett; Matthew L. Maddess; James C. Anderson; Paul E. Brennan; Michael W. Cappi; Jag P. Heer; Celine Helgen; Masakuni Kori; Cyrille Kouklovsky; Stephen P. Marsden; Joanne Norman; David P. Osborn; Maria A. Palomero; John B. J. Pavey; Catherine Pinel; Lesley A. Robinson; Jurgen Schnaubelt; James S. Scott; Christopher D. Spilling

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Total Synthesis of Rapamycin

机译：雷帕霉素的全合成

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For over 30 years, rapamycin has generated a sustained and intense interest from the scientific community as a result of its exceptional pharmacological properties and challenging structural features. In addition to its well known therapeutic value as a potent immunosuppressive agent, rapamycin and its derivatives have recently gained prominence for the treatment of a wide variety of other human malignancies.Herein we disclose full details of our extensive investigation into the synthesis of rapamycin that culminated in a new and convergent preparation featuring a macro-etherification/catechol-templating strategy for construction of the macrocyclic core of this natural product.

机译：30多年来，雷帕霉素因其卓越的药理特性和具有挑战性的结构特征而引起了科学界的持续关注。雷帕霉素及其衍生物除了作为有效的免疫抑制剂具有众所周知的治疗价值外，最近在治疗其他多种人类恶性肿瘤方面也日益受到关注。在此，我们公开了对雷帕霉素合成的广泛研究的全部细节，最终达到了顶峰。在一项新的融合式制备方法中，采用了宏醚化/邻苯二酚-模板化策略来构建这种天然产物的大环核心。

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《Chemistry: A European journal》 |2009年第12期|共41页
作者
Steven V. Ley; Miles N. Tackett; Matthew L. Maddess; James C. Anderson; Paul E. Brennan; Michael W. Cappi; Jag P. Heer; Celine Helgen; Masakuni Kori; Cyrille Kouklovsky; Stephen P. Marsden; Joanne Norman; David P. Osborn; Maria A. Palomero; John B. J. Pavey; Catherine Pinel; Lesley A. Robinson; Jurgen Schnaubelt; James S. Scott; Christopher D. Spilling;
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正文语种 eng
中图分类应用化学;
关键词
anticancer agents; immunosuppressive agents; macrocyclization; natural products; total synthesis;

机译：抗癌剂;免疫抑制剂;大环化;天然产物;全合成;

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1. Total Synthesis of Rapamycin [J] . Steven V. Ley, Miles N. Tackett, Matthew L. Maddess, Chemistry: A European journal . 2009,第12期

机译：雷帕霉素的全合成
2. Total synthesis studies on macrocyclic pipecolic acid natural products: FK506, the antascomicins and rapamycin. [J] . Maddess ML, Tackett MN, Ley SV Progress in drug research. . 2008,第0期

机译：大环哌酸天然产物：FK506，安坦霉素和雷帕霉素的全合成研究。
3. Total Synthesis of Rapamycin [J] . Matthew L. Maddess, Miles N. Tackett, Hidenori Watanabe, Angewandte Chemie . 2007,第4期

机译：雷帕霉素的全合成
4. Inhibition of Target of Rapamycin in Chlamydomonas reinhardtii: simultaneous analysis of the redox-, phospho-, and total proteome [C] . Emily G. Werth, Silas P. Rodrigues, William O. Slade, ASMS Conference on Mass Spectrometry and Allied Topics . 2014

机译：抑制雷纳米蛋白Reinhardtii雷帕霉素的靶向：同时分析氧化还原，磷酸 - 和总蛋白质组
5. Studies towards the total synthesis of rapamycin. [D] . Wang, Tong. 2002

机译：对雷帕霉素全合成的研究。
6. Brain Protein Synthesis Rates in the UM-HET3 Mouse Following Treatment With Rapamycin or Rapamycin With Metformin [O] . Justin J Reid, Melissa A Linden, Frederick F Peelor, -1

机译：雷帕霉素或雷帕霉素二甲双胍治疗后UM-HET3小鼠的脑蛋白合成速率
7. Convergency and Divergency as Strategic Elements in Total Synthesis: The Total Synthesis of (−)-Drupacine and the Formal Total Synthesis of (±)-Cephalotaxine, (−)-Cephalotaxine, and (+)-Cephalotaxine [O] . Liu Qi, Ferreira Eric M., Stoltz Brian M. 2007

机译：收敛性和发散性是总合成中的战略要素：（-）-杜拉帕汀的总合成和（±）-头孢他辛，（-）-头孢他辛和（+）-头孢他定的形式的总合成

Total Synthesis of Rapamycin

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