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    Preparation of (.+-.) 4-demethoxy-6 (and-11-)-deoxydaunomycinone
    1.
    发明授权
    Preparation of (.+-.) 4-demethoxy-6 (and-11-)-deoxydaunomycinone 失效
    （+/-）4-脱甲氧基-6（和 - 11 - ） - 脱氧果阿霉素酮的制备

    公开(公告)号：US4600537A

    公开(公告)日：1986-07-15

    申请号：US599015

    申请日：1984-04-11

    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 ,  C07C49/423 ,  C07D307/89

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

    摘要： (.+-.)4-demethoxy-6(and-11-)-deoxydaunomycinone which are starting materials for anthracycline antitumor antibiotics are prepared by reacting 1,2,3,6-tetrahydrophthalic anhydride with an alcohol of the formula ROH, wherein R is lower alkyl, substituted lower alkyl or aryl to form a monoester, subjecting the monoester to a Friedel-Crafts reaction with acetyl chloride, followed by mild alkaline treatment, to give the corresponding .alpha.,.beta. unsaturated ketone, catalytically reducing same to form the corresponding 4-acetyl-perhydrophthalate reacting the latter with 1,4-dimethoxynaphthalone in the presence of tritluoroacetic anhydride and trifluoroacetic acid to form a mixture of two isomeric compounds, submitting said mixture of isomers to a catalytic reduction of the benzylic carbonyl function, followed by treatment thereof with sulphuric acid at room temperature to afford a mixture of tetracyclic isomers, treating the mixture of tetracyclic isomers with sulphuric acid at 80.degree. C. for one hour to give a 1:1 mixture of the racemic anthracyclinones above mentioned.

    摘要翻译： 通过使1,2,3,6-四氢邻苯二甲酸酐与式ROH的醇反应，制备作为蒽环类抗肿瘤抗生素原料的（+/-）4-脱甲氧基-6（和-11-） - 脱氧余甘杆菌酮，其中R 是低级烷基，取代的低级烷基或芳基以形成单酯，使单酯与乙酰氯进行Friedel-Crafts反应，然后进行温和的碱处理，得到相应的α，β不饱和酮，催化还原形成相应的 4-乙酰基 - 过氢邻苯二甲酸酐与后者与1,4-二甲氧基萘酮在三氟乙酸酐和三氟乙酸的存在下反应形成两种异构化合物的混合物，将所述异构体混合物引入苄羰基官能团的催化还原， 用硫酸在室温下反应，得到四环异构体的混合物，用硫酸在80℃处理四环异构体的混合物， 1小时，得到上述外消旋蒽环霉素的1:1混合物。

    The process for preparing 6-deoxynthracyclines
    4.
    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）。

    Anthracycline glycosides use and compositions containing same
    5.
    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。

    Anthracycline glycosides, use and compositions containing same
    7.
    发明授权
    Anthracycline glycosides, use and compositions containing same 失效
    蒽环类苷，用途和含有它们的组合物

    公开(公告)号：US4563444A

    公开(公告)日：1986-01-07

    申请号：US621681

    申请日：1984-06-18

    申请人： Francesco Angelucci ,  Sergio Penco ,  Federico Arcamone

    发明人： Francesco Angelucci ,  Sergio Penco ,  Federico Arcamone

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

    CPC分类号： C07H15/252 ,  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。

    9-Deoxy-9,10-epoxide-daunomycinone
    8.
    发明授权
    9-Deoxy-9,10-epoxide-daunomycinone 失效
    9-脱氧-9,10-环氧化物 - 道诺霉素酮

    公开(公告)号：US4229355A

    公开(公告)日：1980-10-21

    申请号：US33995

    申请日：1979-04-27

    申请人： Sergio Penco ,  Fausto Gozzi ,  Francesco Angelucci ,  Federico Arcamone

    发明人： Sergio Penco ,  Fausto Gozzi ,  Francesco Angelucci ,  Federico Arcamone

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07D303/32 ,  C07D319/08 ,  C07H15/252

    CPC分类号： C07H15/252 ,  C07D303/32 ,  C07D319/08 ,  Y10S514/908

    摘要： Compounds having the formula: ##STR1## wherein (a) whenR.sup.1 is --COCH.sub.3 or --COCH.sub.2 OH,R.sup.2 is --OH, R.sup.3 is --OCH.sub.3 and R.sup.4 is --H;(b) whenR.sup.2 is --COCH.sub.3 or --COCH.sub.2 OH;R.sup.1 is --OH, R.sup.3 is --H and R.sup.4 is --OCH.sub.3 ;and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyl daunorubicin, a known compound. The invention described herein was made in the course of work under a grant from the United States Department of Health, Education and Welfare.

    摘要翻译： 具有下式的化合物：其中（a）当R 1是-COCH 3或-COCH 2 OH时，R 2是-OH，R 3是-OCH 3，且R 4是-H; （b）当R 2为-COCH 3或-COCH 2 OH时; R1是-OH，R3是-H，R4是-OCH3; 并且其可用于治疗某些哺乳动物肿瘤，由已知化合物9,10-脱氢-N-三氟乙酰柔红霉素制备。 本文描述的发明是在美国卫生，教育和福利部授予的工作过程中作出的。