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1.发明授权
公开(公告)号：US4325946A
公开(公告)日：1982-04-20
申请号：US182119
申请日：1980-08-28
IPC分类号： C07H5/06 , A61K31/70 , A61K31/7008 , A61K31/7024 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07H13/08 , C07H15/252 , A61K31/71 , C07H15/22 , C07H15/24
CPC分类号： C07H13/08 , C07H15/252 , Y02P20/55
摘要： Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxy, one of R.sub.1 and R.sub.2 is methyl and the other of R.sub.1 and R.sub.2 is hydroxy, and pharmaceutically acceptable acid addition salts thereof, which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with certain novel sugars in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form the corresponding protected glycosides from which the protecting groups are removed. This gives the compounds wherein R is hydrogen. The former are converted to the corresponding hydroxyl compounds by treatment with bromine and sodium formate.
摘要翻译： 其中R为氢或羟基的式I的蒽环酸苷，R 1和R 2之一为甲基，R 1和R 2中的另一个为羟基，以及其药学上可接受的酸加成盐，其可用于治疗某些哺乳动物肿瘤 通过在惰性有机溶剂中和在可溶性银盐和脱水剂的存在下将道诺霉素酮与某些新型糖缩合形成保护基被除去的相应的保护的糖苷来制备。 这得到其中R是氢的化合物。 前者通过用溴和甲酸钠处理而转化为相应的羟基化合物。
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公开(公告)号：US4112076A
公开(公告)日：1978-09-05
申请号：US675696
申请日：1976-04-09
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , G04B37/00 , C07H15/24
CPC分类号： C07H15/252 , C07H5/06 , G04B37/0025 , Y02P20/55 , Y10S514/908
摘要： Disclosed is a process for preparing glycoside antitumor antibiotics, including the known compounds daunomycin, adriamycin, 4'-epi-daunomycin and 4'-epi-adriamycin and the novel antibiotics, 3',4'-epi-6'-hydroxydaunomycin, 3',4'-epi-6'-hydroxyadriamycin. 3',4'-epi-daunomycin, 3',4'-epi-adriamycin, 4-demethoxy-4'-epi-daunomycin and 4-demethoxy-4'-epi-adriamycin. Process involves reacting daunomycinone or 4-demethoxy-daunomycinone with a protected 1-halo derivative of 3,4-epi-6-hydroxydaunosamine, 3,4-epi-daunosamine or 4-epi-daunosamine in an inert solvent in the presence of a soluble silver salt catalyst to form a protected derivative of the glycoside antibiotic and removing the protecting groups.
摘要翻译： 公开了一种制备糖苷抗肿瘤抗生素的方法，包括已知的化合物道诺霉素，阿霉素，4'-表柔比星霉素和4'-表阿霉素，以及新型抗生素3'，4'-表 - 6'-羟基天然霉素3 '，4'-表6-hydroxydriamycin。 3'，4'-表柔比星霉素，3'，4'-表阿霉素，4-脱甲氧基-4'-表柔比星霉素和4-脱甲氧基-4'-表阿霉素。 方法包括使道诺霉素酮或4-脱甲氧基道诺霉素酮与3,4-外延-6-羟基丹酰胺，3,4-外延诺胺或4-外 - 柔红霉素的保护的1-卤代衍生物在惰性溶剂中，在 可溶性银盐催化剂以形成糖苷抗生素的被保护的衍生物并除去保护基团。
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公开(公告)号：US4039663A
公开(公告)日：1977-08-02
申请号：US560105
申请日：1975-03-19
IPC分类号： C07H13/04 , C07H15/252 , A61K31/71 , C07H11/00
CPC分类号： C07H13/04 , C07H15/252 , Y10S514/908
摘要： The known antibiotic daunomycin, and the novel compounds daunomycin-.beta.-anomer and 4'-epidaunomycin (both .alpha.- and .beta.-anomers) are prepared by condensing daunomycinone with reactive novel intermediates which are 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxo (or arabino) hexopyranoses.
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公开(公告)号：US4067969A
公开(公告)日：1978-01-10
申请号：US722689
申请日：1976-09-13
IPC分类号： A61K31/35 , A61K31/351 , A61K31/65 , A61K31/704 , A61P35/00 , A61P35/02 , C07D309/14 , C07H13/04 , C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H13/04 , C07D309/14 , C07H15/252 , Y02P20/55 , Y10S514/908
摘要： The novel compounds, 4'-deoxy-daunomycin and 4'-deoxy-adriamycin, as well as derivatives thereof are useful as anti-tumor antibiotics. These compounds are prepared by condensing the corresponding aglycone with a novel trifluoracetyl protected reactive halo sugar which is 2,3,4,6-tetradeoxy-3-trifluoroacetamido-L-threo-hexopyranosyl chloride.
摘要翻译： 新型化合物4'-脱氧 - 道诺霉素和4'-脱氧阿霉素及其衍生物可用作抗肿瘤抗生素。 这些化合物通过将相应的糖苷配基与2,3,4,6-四脱氧-3-三氟乙酰胺基-L-苏 - 六吡喃葡萄糖氯化物的新型三氟乙酰基保护的反应性卤代糖缩合来制备。
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公开(公告)号：US4098798A
公开(公告)日：1978-07-04
申请号：US823581
申请日：1977-08-11
IPC分类号： C07H15/252 , C07D317/10
CPC分类号： C07H15/252
摘要： The known antibiotics adriamycin and its .beta.-anomer, and the novel compounds, 4'-epiadriamycin (both .alpha.- and .beta.-anomers) are prepared by condensing a novel, reactive protected derivative of adriamycinone with reactive intermediates which are 1-halo-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxo (or arabino) hexopyranoses.
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公开(公告)号：US4058519A
公开(公告)日：1977-11-15
申请号：US560104
申请日：1975-03-19
IPC分类号： C07H15/24 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252
CPC分类号： C07H15/252 , Y02P20/55 , Y10S514/908
摘要： The known antitumor antibiotic adriamycin and its .beta.-anomer, and the novel compounds, 4'-epiadriamycin (both .alpha.- and .beta.-anomers) are prepared by condensing a novel, reactive protected derivative of adriamycinone with reactive intermediates which are 1-halo-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxo (or arabino) hexopyranoses.
摘要翻译： 已知的抗肿瘤抗生素阿霉素及其β-对映体，以及新型化合物4'-表阿霉素（α-和β-共聚物两者）均通过将一种新型的反应性保护的阿霉素衍生物与1-卤代 - 2,3,6-三脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基-α--L-赖克（或阿拉伯）六吡喃糖。
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7.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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8.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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公开(公告)号：US4276289A
公开(公告)日：1981-06-30
申请号：US131035
申请日：1980-03-17
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.
摘要翻译： 通过将道诺霉素酮与新的糖4-O-甲基-2,3,3-四氢呋喃缩合来制备其中R为氢或羟基的式I的蒽环酸苷及其盐酸盐，其可用于治疗某些哺乳动物肿瘤 ，6-三脱氧-3-三氟乙酰胺六溴代吡喃葡萄糖氯化物在惰性有机溶剂中，在可溶性银盐和脱水剂存在下反应形成3'，4'-二甲基-4'-O-甲基-N-三氟乙酰柔红霉素，并除去 N-三氟乙酰基。 这得到其中R是氢的化合物。 前者通过常规方法转化成相应的羟基化合物。
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公开(公告)号：US4125607A
公开(公告)日：1978-11-14
申请号：US737473
申请日：1976-11-01
IPC分类号： A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Disclosed is a class of novel daunosaminyl anthracyclinones which are useful in treating Sarcoma 180 ascites.
摘要翻译： 公开了一类可用于治疗肉瘤180腹水的新型氨基甲酰基蒽环类抗生素。
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