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1. 发明申请

WO2003057896A1 METHODS FOR PREPARING ANTHRACYCLINONE DERIVATIVES AND ANTHRACYCLINONE DERIVATIVES PER SE 审中-公开
标题翻译：方法制备蒽环类衍生物和蒽醌衍生物
公开(公告)号：WO2003057896A1
公开(公告)日：2003-07-17
申请号：PCT/US2002/041603
申请日：2002-12-23
申请人： ALBANY MOLECULAR RESEARCH, INC. , MICHELS, Peter, C. , RICH, Joseph, O. , MECKLER, Harold , COTTERILL, Ian
发明人： MICHELS, Peter, C. , RICH, Joseph, O. , MECKLER, Harold , COTTERILL, Ian
IPC分类号： C12P19/56
CPC分类号： C12P19/56 , C07H13/06 , C07H15/252 , C12P7/62 , C12P7/66
摘要： The present invention relates to a process for preparation of a product compound of the Formula (I), where R 1 is an acyl group, R 2 is H, an N-alkylated amino sugar, or a non-basic sugar moiety, and R 3 is H, OH, or OCH 3 . The process involves reacting a starting compound of the Formula (II) with an acyl donor compound in the presence of a non-chemically modified lipase, under conditions effective to produce the product compound. Another aspect of the present invention relates to a compound of the following Formula (III), where: R 1 is an acyl radical of a carboxylic acid selected from the group consisting of: polyethylene glycol acetic acid and polyunsaturated fatty acid; and R 2 = 2,6-dideoxy-2-fluoro-α-talopyranosyl; 3-trifluoroacetylamino-2,3,6-trideoxy-α-L- lyxo -hexopyranosyl; or 3-deamino-3-(2'-pyrroline-1'-yl)-2,3,6-trideoxy-α-L- lyxo -hexopyranosyl; or a pharmaceutically acceptable salt thereof. The present invention also relates to a compound of the Formula (IV) where n is 4 or 5, or a pharmaceutically acceptable salt thereof. Another aspect of the present invention relates to a compound of the Formula (V) where: R 1 is an acyl group, R 2 is 3-substituted allyloxycarbonylamino-2,3,6-trideoxy-α-L- lyxo -hexopyranosyl, R 3 is H, OH, or OCH 3 .
摘要翻译：本发明涉及一种制备式（I）的产物化合物的方法，其中R 17是酰基，R 2b是H，N- 烷基化氨基糖或非碱性糖部分，R 3是H，OH或OCH 3 S 3。该方法包括在非化学修饰的脂肪酶存在下，在有效产生产物化合物的条件下使式（II）的起始化合物与酰基供体化合物反应。本发明的另一方面涉及下式（III）的化合物，其中：R 1是选自以下的羧酸的酰基：聚乙二醇乙酸和多不饱和的脂肪酸; 和R 2 = 2,6-二脱氧-2-氟-α-三氟乙酸; 3-三氟乙酰氨基-2,3,6-三脱氧谷氨酸; L-赖氨酸 - 六吡喃葡糖基; 或3-脱氨基-3-（2'-吡咯啉-1-基） - 基）-2,3,6-三脱氧-α-和L-赖氨酸 - 六吡喃葡糖基; 或其药学上可接受的盐。本发明还涉及其中n为4或5的式（IV）化合物或其药学上可接受的盐。本发明的另一方面涉及式（V）的化合物，其中：R 1是酰基，R b 2是3-取代的烯丙氧基羰基氨基-2,3 ，6-三脱氧-L-赖氨酸 - 六吡喃葡糖基，R 3是H，OH或OCH 3 S 3。

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