基本信息:
- 专利标题： SYNTHESIS OF TETRACYCLINES AND INTERMEDIATES THERETO
- 专利标题（中）：四氯乙烯的合成及其中间体
- 申请号：PCT/US2010/001284 申请日：2010-04-30
- 公开(公告)号：WO2010126607A2 公开(公告)日：2010-11-04
- 发明人： MYERS, Andrew, G. , KUMMER, David, A. , LI, Derun , HECKER, Evan , DION, Amelie , WRIGHT, Peter, Maughan
- 申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE , MYERS, Andrew, G. , KUMMER, David, A. , LI, Derun , HECKER, Evan , DION, Amelie , WRIGHT, Peter, Maughan
- 申请人地址： 17 Quincy Street Cambridge, MA 02138 US
- 专利权人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE,MYERS, Andrew, G.,KUMMER, David, A.,LI, Derun,HECKER, Evan,DION, Amelie,WRIGHT, Peter, Maughan
- 当前专利权人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE,MYERS, Andrew, G.,KUMMER, David, A.,LI, Derun,HECKER, Evan,DION, Amelie,WRIGHT, Peter, Maughan
- 当前专利权人地址： 17 Quincy Street Cambridge, MA 02138 US
- 代理机构： BAKER, Hunter, C.
- 优先权： US61/322,613 20100409; US61/174,185 20090430
- 主分类号： C07C237/26
- IPC分类号： C07C237/26
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 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（中）：
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已经导致了以前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高效合成以前从未制备的新型四环素类似物。 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位置的取代基。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07C | 无环或碳环化合物 |
| ------C07C237/00 | 羧酸酰胺，酸部分的碳架进一步被氨基取代 |
| --------C07C237/02 | .羧酰胺基的碳原子连接在碳架的非环碳原子上 |
| ----------C07C237/26 | ..其环是至少由4个环组成的稠环系的组成部分，例如四环素 |