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    The process for preparing 6-deoxynthracyclines
    51.
    发明授权
    The process for preparing 6-deoxynthracyclines 失效
    6-脱氧蒽环的制备方法

    公开(公告)号：US4939282A

    公开(公告)日：1990-07-03

    申请号：US622177

    申请日：1984-06-19

    申请人： Francesco Angelucci ,  Sergio Penco ,  Ermes Vanotti ,  Federico Arcamone

    发明人： Francesco Angelucci ,  Sergio Penco ,  Ermes Vanotti ,  Federico Arcamone

    IPC分类号： C07C50/38 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07C45/00 ,  C07C46/00 ,  C07C50/36 ,  C07C67/00 ,  C07D407/04 ,  C07H15/252

    CPC分类号： C07D407/04 ,  C07H15/252

    摘要： A new process for the preparation of 6-deoxyanthracyclinones of general formula I: ##STR1## wherein R represents a hydrogen atom, a hydroxy group or a lower alkoxy group is described. The process provides a total synthesis of the 6-deoxyanthracyclinones of formula I using 1,2,3,6-tetrahydro-phthalate as starting material. The obtained racemic mixture of the compounds of formula I, if desired, can be submitted to optical resolution by the conventional method of conversion to diastereomeric derivatives using a chiral resolving agent. Alternatively, the racemic mixture can be used as such for the condensation with a suitably protected halosugar derivative to obtain alpha glycosidic derivatives of formula XV: ##STR2## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolisis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.

    摘要翻译： 描述了制备通式I的6-脱氧尿嘧啶的新方法：其中R表示氢原子，羟基或低级烷氧基。 该方法提供使用1,2,3,6-四氢邻苯二甲酸酯作为起始原料的式I的6-脱氧蒽环类的全合成。 如果需要，所得到的式I化合物的外消旋混合物可以通过使用手性拆分剂转化成非对映体衍生物的常规方法进行光学拆分。 或者，外消旋混合物可以直接用于与适当保护的卤糖衍生物的缩合，以获得式XV的α糖苷衍生物：其中R 1表示氢原子或羟基，R 2和R 3之一表示 氢原子，R2和R3中的另一个表示氢原子或羟基，X是氢原子或三氟乙酰基。 式XV的α-糖苷类的N-三氟乙酰基7S：9S和7R：9R衍生物可以通过硅胶色谱分离，得到在温和的碱性水解后，所需的7S：9Sα-糖苷（R1 = H）为游离 碱，并且最终可以通过已知的方法转化成它们相应的多柔比星衍生物（R1 = OH）。

    6-amino anthracyclines, process for their preparation and use thereof
    52.
    发明授权
    6-amino anthracyclines, process for their preparation and use thereof 失效
    6-氨基蒽环霉素，其制备及使用方法

    公开(公告)号：US4891360A

    公开(公告)日：1990-01-02

    申请号：US73109

    申请日：1987-07-14

    申请人： Francesco Angelucci ,  Mauro Gigli ,  Sergio Penco

    发明人： Francesco Angelucci ,  Mauro Gigli ,  Sergio Penco

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252

    CPC分类号： C07H15/252

    摘要： Anthracycline glycosides having the general formula (A): ##STR1## wherein R.sub.1 is hydrogen, hydroxy or methoxy; R.sub.2 is amino, R.sub.3 is hydrogen or hydroxy and X is hydrogen; and their pharmaceutically acceptable salts; are antitumor agents. The compounds are obtained by reduction of the corresponding 6-nitro derivatives with stannous chloride in presence of sodium acetate or with palladium or charcoal in presence of cyclohexene.

    摘要翻译： 具有通式（A）的蒽环酸苷：其中R1是氢，羟基或甲氧基; R2是氨基，R3是氢或羟基，X是氢; 及其药学上可接受的盐; 是抗肿瘤剂。 该化合物是通过在乙酸钠存在下用氯化亚锡或在环己烯存在下用钯或炭还原相应的6-硝基衍生物而获得的。

    Anthracycline glycosides use and compositions containing same
    55.
    发明授权
    Anthracycline glycosides use and compositions containing same 失效
    蒽环类苷用途及其含有的组合物

    公开(公告)号：US4465671A

    公开(公告)日：1984-08-14

    申请号：US382144

    申请日：1982-05-26

    申请人： Francesco Angelucci ,  Sergio Penco ,  Federico Arcamone

    发明人： Francesco Angelucci ,  Sergio Penco ,  Federico Arcamone

    IPC分类号： C07C50/38 ,  C07H15/252 ,  A61K31/71 ,  C07H15/24

    CPC分类号： C07H15/252 ,  C07C50/38 ,  Y02P20/55

    摘要： Anthracycline glycosides of the formula (I) ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is hydroxy, each of R.sub.3, R.sub.4 and R.sub.5 is independently selected from the group consisting of hydrogen and hydroxy and X is hydrogen or trifluoroacetyl, with the provisos that R.sub.4 and R.sub.5 are not simultaneously hydroxy and that if R.sub.3 is hydroxy, then X is hydrogen, which are useful in treating certain mammalian tumors are prepared by condensing an aglycone of the formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are defined as above, with a suitable protected halosugar, after which the protecting groups are removed.

    摘要翻译： 式（I）的蒽环酸糖苷其中R 1和R 2之一是氢，R 1和R 2中的另一个是羟基，R 3，R 4和R 5各自独立地选自氢和羟基，X 是氢或三氟乙酰基，条件是R 4和R 5不同时为羟基，如果R 3为羟基，则X为氢，其可用于治疗某些哺乳动物肿瘤通过将式（II）的糖苷配基缩合制备其中R 1和R 2如上所定义，具有合适的受保护的卤糖，之后除去保护基。

    Process for preparing daunomycin and analogues thereof
    60.
    发明授权
    Process for preparing daunomycin and analogues thereof 失效
    道诺霉素及其类似物的制备方法

    公开(公告)号：US4107423A

    公开(公告)日：1978-08-15

    申请号：US695434

    申请日：1976-08-14

    申请人： Federico Arcamone ,  Luigi Bernardi ,  Bianca Patelli ,  Sergio Penco

    发明人： Federico Arcamone ,  Luigi Bernardi ,  Bianca Patelli ,  Sergio Penco

    IPC分类号： C07H15/252 ,  C07H15/24

    CPC分类号： C07H15/252

    摘要： Racemic anthracyclinones of the general formula II ##STR1## when condensed with 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxo-pyranosyl chloride in the presence of silver trifluoromethane sulphonate yield an easily separable mixture of equimolar amounts of exclusively the .alpha.-glycoside of the 7S : 9S diastereomer and the .beta.-glycoside of the 7R : 9R diastereomer. In this way the biologically important .alpha.-glycosides of the 7S : 9S diastereomer of the general formula I (below) are easily prepared from a racemic anthracyclinone.

    摘要翻译： 在三氟甲磺酸银存在下与2,3,6-三脱氧-3-三氟乙酰胺基-4-0-三氟乙酰-α-L-吡唑并吡喃二氯甲烷缩合时，通式II II的外消旋蒽环类产生容易 7S：9S非对映异构体的α-糖苷和7R：9R非对映异构体的β-糖苷的等摩尔量的可分离混合物。 以这种方式，通式I（下文）的7S：9S非对映异构体的生物学上重要的α-糖苷类可以容易地由外消旋​​蒽环类抗生素制备。