公开(公告)号：EP1044209A1

公开(公告)日：2000-10-18

申请号：EP98959481.7

申请日：1998-11-17

申请人： Abbott Laboratories

发明人： KU, Yi-Yin ,  RILEY, David, A. ,  LEE, Elaine, C. ,  TIEN, Jien-Heh, J.

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： The claimed invention provides a novel method of preparing 6-O-methyl erythromycin A. The process comprises the steps of reducing the 9-keto group of erythromycin A to form a 9-hydroxy erythromycin A, protecting the 9-, 2'-, and/or 4'-hydroxyl groups of erythromycin A, selectively methylating the 6-position of the 9-hydroxy erythromycin A derivative, deprotecting the hydroxyl groups and oxidizing the 9-hydroxyl to afford 6-O-methyl erythromycin A.

摘要翻译： 本发明提供了一种制备6-O-甲基红霉素A的新方法。该方法包括将红霉素A的9-酮基还原成9-羟基红霉素A，保护9-，2'-， 和/或红霉素A的4'-羟基，选择性甲基化9-羟基红霉素A衍生物的6-位，使羟基脱保护并氧化9-羟基，得到6-O-甲基红霉素A.

公开(公告)号：EP1044209B1

公开(公告)日：2004-08-18

申请号：EP98959481.7

申请日：1998-11-17

申请人： Abbott Laboratories

发明人： KU, Yi-Yin ,  RILEY, David, A. ,  LEE, Elaine, C. ,  TIEN, Jien-Heh, J.

IPC分类号： C07H17/08

CPC分类号： C07H17/08

公开(公告)号：EP0781261A2

公开(公告)日：1997-07-02

申请号：EP95933078.0

申请日：1995-09-14

申请人： Abbott Laboratories

发明人： CHORGHADE, Mukund, S. ,  DOLPHIN, David, H. ,  HILL, David, R. ,  HINO, Fumio ,  LEE, Elaine, C.

IPC分类号： G01N33 ,  B01J31 ,  C07B33 ,  C07D231 ,  C07D233 ,  C07D405 ,  C07D413 ,  C07D487

CPC分类号： B01J31/1815 ,  B01J2531/025 ,  B01J2531/16 ,  B01J2531/62 ,  B01J2531/72 ,  B01J2531/821 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07B33/00 ,  C07D231/44 ,  C07D233/36 ,  C07D405/04 ,  C07D413/04

摘要： A method for the systematic and efficient synthetic preparation and identification of metabolites of a pharmaceutical product in order to study possible toxic and/or otherwise biologically-active metabolites of such pharmaceutical products as early and conveniently as possible in the very expensive drug development process, comprising adding samples of the pharmaceutical product to a series of combinations of a synthetic metalloporphyrin (SMP) with a synthetic metalloporphyrin-co-oxidizing reagent in the presence of a suitable solvent, under specified conditions, in a manner such that each sample of pharmaceutical product is reacted with a different combination of synthetic metalloporphyrin, SMP-co-oxidizing reagent and solvent, followed by separation and isolation of the resulting oxidative products, then confirmation of the identity of metabolites from the pre-identified oxidative products by appropriate animal model studies, and subjecting the actual metabolites prepared in larger quantities by the above method to toxicologic, pathologic, histopathologic, mechanistic or genotoxic testing in order to identify toxic and/or otherwise metabolically-active beneficial or detrimental individual metabolites.