公开(公告)号：EP2424834A2

公开(公告)日：2012-03-07

申请号：EP10717900.4

申请日：2010-04-30

申请人： President and Fellows of Harvard College

发明人： MYERS, Andrew, G. ,  KUMMER, David, A. ,  LI, Derun ,  HECKER, Evan ,  DION, Amelie ,  WRIGHT, Peter, Maughan

IPC分类号： C07C237/26

CPC分类号： C07D261/20 ,  C07B2200/07 ,  C07C29/32 ,  C07C45/00 ,  C07C45/29 ,  C07C45/67 ,  C07C45/673 ,  C07C45/69 ,  C07C49/637 ,  C07C237/26 ,  C07C311/05 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2603/46 ,  C07C2603/66 ,  C07D207/16 ,  C07D209/58 ,  C07D213/30 ,  C07D213/74 ,  C07D233/61 ,  C07D261/18 ,  C07D277/24 ,  C07D277/64 ,  C07D295/15 ,  C07D295/155 ,  C07D498/04 ,  C07F7/0814 ,  C07F7/188

摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously thought susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

摘要翻译： 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加导致了以前认为易受四环素抗生素影响的许多生物体之间的抵抗。 通过手性烯酮中间体最近开发的四环素类似物的模块合成使得能够有效合成以前从未制备的新的四环素类似物。 本发明提供了更有效的制备烯酮中间体的途径，并允许四环素环体系的4a，5,5a和12a的取代基。

公开(公告)号：EP2424834B1

公开(公告)日：2018-07-11

申请号：EP10717900.4

申请日：2010-04-30

申请人： President and Fellows of Harvard College

发明人： MYERS, Andrew, G. ,  KUMMER, David, A. ,  LI, Derun ,  HECKER, Evan ,  DION, Amelie ,  WRIGHT, Peter, Maughan

IPC分类号： C07C237/26 ,  C07D295/155 ,  C07D233/61 ,  C07C311/05 ,  C07D213/74 ,  C07D207/16 ,  C07D295/15 ,  C07D209/58 ,  C07C49/637 ,  C07D261/20 ,  C07F7/08 ,  C07C45/67 ,  C07C45/69 ,  C07C49/623 ,  C07D277/64 ,  C07D498/04 ,  C07D277/24 ,  C07D213/30 ,  A61P31/04 ,  A61K31/65

CPC分类号： C07D261/20 ,  C07B2200/07 ,  C07C29/32 ,  C07C45/00 ,  C07C45/29 ,  C07C45/67 ,  C07C45/673 ,  C07C45/69 ,  C07C49/637 ,  C07C237/26 ,  C07C311/05 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2603/46 ,  C07C2603/66 ,  C07D207/16 ,  C07D209/58 ,  C07D213/30 ,  C07D213/74 ,  C07D233/61 ,  C07D261/18 ,  C07D277/24 ,  C07D277/64 ,  C07D295/15 ,  C07D295/155 ,  C07D498/04 ,  C07F7/0814 ,  C07F7/188

摘要： The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously thought susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.