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11. 发明授权

US4155911A Process for the production of substituted 4-thia-2,6-diaza[3.2.0]-2-heptene-7-one 失效
标题翻译：制备取代的4-硫杂-2,6-二氮杂{8 3.2.0 {9,2-庚烯-7-酮
公开(公告)号：US4155911A
公开(公告)日：1979-05-22
申请号：US820895
申请日：1977-08-01
申请人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
发明人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
IPC分类号： C07D205/08 , C07D513/04
CPC分类号： C07D513/04 , C07D205/08
摘要： A new process is disclosed for the preparation of compounds of structure: ##STR1## and are as defined herein characterized in that a compound of structure ##STR2## where R and R.sup.1 have the meanings given herein, is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of structure: ##STR3## where R and R.sup.1 have the meanings given herein, Hal is a halogen atom; THE INTERMEDIATE COMPOUND (III) in a suitable solvent is then reacted with an appropriate nucleophilic reagent to obtain the compound IV where Z replaces Hal, where Z is defined herein;The compound (IV) is then subjected to an allylic halogenation in a suitable solvent by reacting it with a haloamide either under the influence of light alone or by heating it in the presence of a free radical initiator, to give a compound of structure: ##STR4## where R, R.sup.1 and Hal and Z have the above meanings; THE INTERMEDIATE COMPOUND (V) is then reacted with a reducing agent to give finally the desired compound (I).
摘要翻译：公开了用于制备结构式（I）的化合物的新方法，其定义如下，其特征在于其中R和R 1具有本文给出的含义的结构式（II）的化合物在在金属氧化物或卤代酰胺的存在下，在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物的存在下，与卤代酰胺合适的溶剂，得到结构化合物（III）其中R和R1具有本文给出的含义，Hal是卤素原子; 然后将合适的溶剂中的中间体化合物（III）与合适的亲核试剂反应，得到Z代替Hal的化合物IV，其中Z在本文中定义; 然后使化合物（IV）在合适的溶剂中通过与单独的光的影响下的卤代酰胺反应或通过在自由基引发剂的存在下加热使其与卤代酰胺反应，得到结构式（V）其中R，R1，Hal和Z具有上述含义; 然后将中间体化合物（V）与还原剂反应，最终得到所需化合物（I）。

12. 发明授权

US4077970A Methyl-.alpha.[3'acetoxy-1'isopropenyl]-3 substituted 1.alpha.,5x-4-thia 2,6 diaza[3,2,0]2-heptene-6 acetate 7-one 失效
标题翻译：甲基 - {60 {8 3 {40乙酰氧基-1 {40异丙烯基{9,3取代的1 {60,5x-4-硫杂-2,6-二氮杂{8 3,2,0 {9 2-庚烯-6-乙酸酯7- 一
公开(公告)号：US4077970A
公开(公告)日：1978-03-07
申请号：US603605
申请日：1975-08-11
申请人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
发明人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
IPC分类号： C07D205/08 , C07D513/04 , C07D513/08
CPC分类号： C07D513/04 , C07D205/08
摘要： A process is disclosed for the preparation of a compound of the formula ##STR1## where R and R.sup.1 are defined herein below, wherein a compound of the structure; ##STR2## is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of the structure; ##STR3## which compound, in a suitable solvent is reacted with a suitable nucleophilic reagent to obtain the compound; ##STR4## which compound is then subjected to allylic halogenation to give a compound of the structure; ##STR5## which is then reacted with a reducing agent to yield I.
摘要翻译：公开了用于制备下式化合物的方法，其中R和R 1如下文所定义，其中该结构的化合物; 在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物或卤代酰胺的存在下，在合适的溶剂中与卤代酰胺反应。，得到结构的化合物; 该化合物在合适的溶剂中与合适的亲核试剂反应得到化合物; 然后将该化合物进行烯丙基卤化，得到结构的化合物; 然后将其与还原剂反应以产生I.

13. 发明授权

US4345070A Process for the preparation of 4'-deoxy-daunorubicin and 4'-deoxy-doxorubicin 失效
标题翻译： 4'-脱氧柔红霉素和4'-脱氧多柔比星的制备方法
公开(公告)号：US4345070A
公开(公告)日：1982-08-17
申请号：US270877
申请日：1981-06-05
申请人： Antonino Suarato , Sergio Penco , Federico Arcamone
发明人： Antonino Suarato , Sergio Penco , Federico Arcamone
IPC分类号： C07D309/14 , A61K31/65 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： A new process for the preparation of the known 4'-deoxydaunorubicin and 4'-deoxydoxorubicin is disclosed. The used starting material is 4'-eip-N-trifluoroacetyldaunorubicin which is converted into 4'-deoxy-4'-iodo-N-trifluoroacetyl-daunorubicin from which 4'-deoxy-daunorubicin can be reductively obtained and eventually transformed, by known methods, into 4'-deoxy-doxorubicin.
摘要翻译：公开了一种制备已知的4'-脱氧柔红霉素和4'-脱氧阿霉素的新方法。所使用的原料是4'-eip-N-三氟乙酰基柔红霉素，其被转化为4'-脱氧-4'-碘-N-三氟乙酰基柔红霉素，从其中可以还原获得4'-脱氧柔红霉素并最终通过已知的方法，进入4'-脱氧 - 多柔比星。

14. 发明授权

US4906743A 4-demethoxy-4-amino-anthracyclines 失效
公开(公告)号：US4906743A
公开(公告)日：1990-03-06
申请号：US181506
申请日：1988-04-14
申请人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
发明人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotized followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

15. 发明授权

US4438105A 4'-Iododerivatives of anthracycline glycosides 失效
标题翻译：蒽环类苷的4'-碘代衍生物
公开(公告)号：US4438105A
公开(公告)日：1984-03-20
申请号：US368415
申请日：1982-04-14
申请人： Antonino Suarato , Sergio Penco , Federico Arcamone , Anna M. Casazza
发明人： Antonino Suarato , Sergio Penco , Federico Arcamone , Anna M. Casazza
IPC分类号： C07H15/24 , A61K31/35 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71
CPC分类号： C07H15/252 , Y10S514/908
摘要： Starting from the known 4'-deoxy-4'-iodo-N-trifluoroacetyldaunorubicin, two new anthracycline glycosidic antibiotics, the 4'-deoxy-4'-iodo-daunorubicin and 4'-deoxy-4'-iodo-doxorubicin, have been prepared by known procedures. Both the new glycosides have been found to be endowed with outstanding antitumoral activity.
摘要翻译：从已知的4'-脱氧-4'-碘-N-三氟乙酰基柔红霉素开始，两种新的蒽环类抗生素，4'-脱氧-4'-碘柔红霉素和4'-脱氧-4'-碘 - 多柔比星，具有通过已知程序制备。这些新的糖苷都被发现具有突出的抗肿瘤活性。

16. 发明授权

US4985548A 4-demethoxy-4-amino-anthracyclines 失效
标题翻译： 4-脱甲氧基-4-氨基蒽环类
公开(公告)号：US4985548A
公开(公告)日：1991-01-15
申请号：US462549
申请日：1990-01-09
申请人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
发明人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C46/00 , C07C50/22 , C07C50/38 , C07C225/34 , C07H15/252
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotised followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

17. 发明授权

US4965351A 4-demethoxy-4-amino-anthracyclines 失效
标题翻译： 4-脱甲氧基-4-氨基蒽环类
公开(公告)号：US4965351A
公开(公告)日：1990-10-23
申请号：US430149
申请日：1989-11-01
申请人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
发明人： Michele Caruso , Antonino Suarato , Francesco Angelucci , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C46/00 , C07C50/22 , C07C50/38 , C07C225/34 , C07H15/252
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotized followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

18. 发明授权

US4477444A Antracycline glycosides, pharmaceutical compositions and method of use 失效
标题翻译：抗菌素苷，药物组合物和使用方法
公开(公告)号：US4477444A
公开(公告)日：1984-10-16
申请号：US434509
申请日：1982-10-15
申请人： Antonino Suarato , Sergio Penco , Federico Arcamone
发明人： Antonino Suarato , Sergio Penco , Federico Arcamone
IPC分类号： C07H15/252 , A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , Y02P20/55
摘要： Disclosed is a process for preparing the new antitumor glycosides: 4'-deoxy-3'-epi-daunorubicin and 4'-deoxy-3'-epi-doxorubicin starting from the known 3'-epi-4'-keto-N-trifluoroacetyl-daunorubicin.Reduction of the 4'-keto group with sodium borohydride to the corresponding 4'-hydroxy group, reacting the so obtained intermediate with trifluoromethanesulphonic anhydride followed by treatment with n-tetrabutylammonium iodide, dehalogenated reductively, by treatment with tributyl tin hydride to 4'-deoxy-3'-epi-N-trifluoroacetyl-daunorubicin.A mild alkaline hydrolysis removes the N-protecting group to give 4'-deoxy-3'-epi-daunorubicin which is successively transformed, via its 14-bromo derivative, in its doxorubicin analogue.
摘要翻译：公开了一种制备新型抗肿瘤糖苷的方法：从已知的3'-表面-4'-酮-n-三磷酸开始制备4'-脱氧-3'-表柔比星和4'-脱氧-3'-表阿霉素，三氟乙酰柔红霉素。将4'-酮基用硼氢化钠还原成相应的4'-羟基，使所得中间体与三氟甲磺酸酐反应，然后用正丁基碘化铵处理，还原脱卤，通过用三丁基锡氢化物处理至4'- 脱氧-3'-表N-N-三氟乙酰柔红霉素。轻度碱性水解除去N-保护基，得到4'-脱氧-3'-表柔比星，其通过其14-溴衍生物在其多柔比星类似物中相继转化。

19. 发明授权

US4143037A Thiohydrazoazetidinones 失效
标题翻译： THIOHYDRAZOAZETIDINONES
公开(公告)号：US4143037A
公开(公告)日：1979-03-06
申请号：US797608
申请日：1977-05-16
申请人： Maurizio Foglio , Giovanni Franceschi , Paolo Masi , Antonino Suarato
发明人： Maurizio Foglio , Giovanni Franceschi , Paolo Masi , Antonino Suarato
IPC分类号： C07D205/095 , C07D205/08
CPC分类号： C07D205/095
摘要： A process is disclosed for preparing compounds of structure: ##STR1## where R.sup.1 is hydroxyl, alkoxy with 1 to 4 carbon atoms, trichloroethoxy, benzyloxy, p-methoxybenzyloxy, p-nitrobenzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, or p-halophenacyloxy;Z is hydrogen, hydroxyl, --O-alkyl, --O--CO-alkyl, --Br, --I, --N.sub.3, --O--CO--CH.sub.3, O--CO--NH.sub.2, or an S-mononuclear heterocyclic ring,Starting from ##STR2## where R is hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenyl-isopropyl, phenoxy-isopropyl, pyridyl-4-thiomethyl, or tetrazolyl-1-methyl;R.sup.2 and R.sup.3 are lower alkyl, a mononuclear aryl ring, CN, a mononuclear heterocyclic ring or the radicals --COR.sup.4, --COOR.sup.4, ##STR3## --CONHR.sup.4, or R.sub.2 and R.sub.3 together represent ##STR4## where T represents ##STR5## and R.sup.4 is a lower alkyl, a mononuclear aryl or heterocyclic ring, WHEREIN THE COMPOUND (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed in an acid medium, and the resultant 3-amino-2-.beta.-thiohydrazoazetidinone: ##STR6## in which R.sup.1, R.sup.2, R.sup.3 and Z have the meanings given heretofore,Is reacted between -100.degree. and +120.degree. C. with inorganic basic or weakly acid oxides or inorganic and organic bases, to give (V).

20. 发明授权

US4012381A Process for preparing cephalosporins and intermediates 失效
标题翻译：制备头孢菌素和中间体的方法
公开(公告)号：US4012381A
公开(公告)日：1977-03-15
申请号：US586376
申请日：1975-06-12
申请人： Maurizio Foglio , Giovanni Franceschi , Paolo Masi , Antonino Suarato
发明人： Maurizio Foglio , Giovanni Franceschi , Paolo Masi , Antonino Suarato
IPC分类号： C07D205/095 , C07D501/08 , C07D501/18 , C07D501/20
CPC分类号： C07D205/095
摘要： A process is disclosed for preparing derivatives of 7-amino-cephalosporanic acid and 7-amino-desacetoxycephalosporanic acid of structure: starting from a 3-acylamino-2.beta.-thiohydrazoazetidinone of structure: ##STR1## wherein the compound (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed with water in an acid medium, and the resultant 3-amino-2.beta.-thiohydrazoazetidinone of structure: ##STR2## is reacted in a suitable solvent and at a temperature between -100.degree. and +120.degree. C with a compound selected from the class consisting of inorganic basic or weakly acid oxides and inorganic and organic bases, to finally give the desired compound (V) which is isolated and purified in known manner.2.beta.-thiohydrazoazetidinones are also disclosed as intermediates.
摘要翻译：公开了一种制备以下结构的3-氨基 - 头孢烷酸和7-氨基 - 脱乙酰氧基头孢烷酸的衍生物的方法，其结构如下：起始于结构如下的3-酰基氨基-2β-硫代代氮杂环丁酮：（II' ），其中化合物（II'）在叔胺存在下与卤化磷反应，相应的亚氨基氯与低级脂族醇反应，所形成的亚氨基醚在酸性介质中用水水解，得到的将结构如下的3-氨基-2β-硫代代代氮杂环丁酮在合适的溶剂中，在-100至+ 120℃的温度下与选自无机碱性或弱碱性的化合物反应酸性氧化物和无机和有机碱，最终得到所需的化合物（V），其以已知方式分离和纯化。

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