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公开(公告)号：US4325947A
公开(公告)日：1982-04-20
申请号：US263002
申请日：1981-05-12
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： A new anthracycline glycoside, which is 4-demethoxy-4'-deoxydoxorubicin, provided with outstanding antitumoral activity also by oral route, has been prepared by condensation of 4-demethoxydaunomycinone with 2,3,4,6-tetradeoxy-3-trifluoroacetamido-L-threo-hexopyranosyl chloride.By elimination of the protecting group from the so obtained glycoside through a mild alkaline hydrolysis, 4-demethoxy-4'-deoxydaunorubicin was obtained which was successively brominated to give the corresponding 14-bromo derivative. By a subsequent hydrolysis with sodium formate the brominated intermediate was transformed into 4-demethoxy-4'-deoxydoxorubicin eventually isolated as its hydrochloride.
摘要翻译： 通过口服途径提供了具有优异抗肿瘤活性的4-脱甲氧基-4'-脱氧阿霉素的新型蒽环苷类糖苷，已经通过4-脱甲氧基多霉素酮与2,3,4,6-四脱氧-3-三氟乙酰氨基 - L-苏 - 六吡喃葡萄糖。 通过轻度碱性水解从所得糖苷中除去保护基，得到4-脱甲氧基-4'-脱氧阿诺醌，依次溴化得到相应的14-溴衍生物。 随后用甲酸钠水解，将溴化中间体转化为最终以其盐酸盐分离的4-脱甲氧基-4'-脱氧阿霉素。
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2.发明授权Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效抗癌蒽环类苷，其制备方法，其中间体及其组合物和用途
公开(公告)号：US4393052A
公开(公告)日：1983-07-12
申请号：US316058
申请日：1981-10-29
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07D309/30 , C07H13/04 , C07H13/06 , C07H15/04 , C07H15/252 , A61K31/71 , C07H15/22
CPC分类号： C07H15/04 , C07D309/30 , C07H13/04 , C07H15/252 , Y10S514/908
摘要： Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosyl chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyranosyl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifluoroacetyl-L-lyxo-hexopyranosyl chloride.
摘要翻译： 通过将道诺霉素与2,3,4,6-四脱氧-4-C-亚甲基-3-三氟乙酰氨基-L-苏 - 己酰氯氯化物缩合制备新型抗肿瘤蒽环类苷; 2,3,4,6-四脱氧-4-C-亚甲基-3-三氟乙酰氨基-L-阿拉伯 - 己酸乳酸酰氯或2,3,6-三脱氧-4-C-三氟乙酰氨基甲基-3-三氟乙酰胺基-3-羟基乙酰氨基 -L-胞嘧啶 - 六吡喃葡糖酰氯。
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3.发明授权Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效抗癌蒽环类苷，其制备方法，其中间体及其组合物和用途
公开(公告)号：US4366149A
公开(公告)日：1982-12-28
申请号：US316057
申请日：1981-10-29
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H13/04 , C07H15/04 , C07H15/252 , C07H5/06 , C07H15/24
CPC分类号： C07H13/04 , C07H15/04 , C07H15/252 , Y10S514/908
摘要： Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-3,4-ditrifluoroacetamido-L-lyxo-[or L-arabino-]hexopyranosyl chloride.
摘要翻译： 通过将道诺霉素酮与2,3,4,6-四脱氧-3,4-二三氟乙酰氨基-L-赖氨酸 - 或[L-阿拉伯糖]六吡喃葡萄糖氯化物缩合来制备新型抗肿瘤蒽环苷。
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