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    Daunomycin analogues, their preparation and use
    1.
    发明授权
    Daunomycin analogues, their preparation and use 失效
    道诺霉素类似物，其制备和用途

    公开(公告)号：US4046878A

    公开(公告)日：1977-09-06

    申请号：US579901

    申请日：1975-05-22

    申请人： Bianca Patelli ,  Luigi Bernardi ,  Federico Arcamone ,  Aurelio Di Marco

    发明人： Bianca Patelli ,  Luigi Bernardi ,  Federico Arcamone ,  Aurelio Di Marco

    IPC分类号： A61K31/704 ,  C07H15/252 ,  A61K31/71 ,  C07H11/00

    CPC分类号： C07H15/252 ,  Y10S514/908

    摘要： Daunomycin analogues of the formula: ##STR1## wherein when each R.sub.1 is hydrogen, each R is hydrogen, chlorine, bromine, methyl or methoxy and when each R.sub.1 is chlorine, bromine or methyl, each R is hydrogen, are useful in treating various mammalian tumors and are prepared by reacting a daunomycinone derivative of the formula: ##STR2## wherein R and R.sub.1 are as defined above with 1-chloro-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxopyranose in an inert anhydrous organic solvent in the presence of a catalyst and a hydrogen chloride acceptor.

    摘要翻译： 道诺霉素类似物，具有下式：其中当每个R 1是氢时，每个R是氢，氯，溴，甲基或甲氧基，并且当每个R 1是氯，溴或甲基时，每个R是氢，可用于 治疗各种哺乳动物肿瘤，并且通过使下式的道诺霉素酮衍生物：其中R和R 1如上所定义的道诺霉素酮衍生物与1-氯-2,3,6-三脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基 α-L-吡喃葡萄糖在惰性无水有机溶剂中，在催化剂和氯化氢受体存在下。

    Process for preparing daunomycin and analogues thereof
    7.
    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。

    Selective demethylation of anthracycline derivatives
    8.
    发明授权
    Selective demethylation of anthracycline derivatives 失效
    蒽环类衍生物的选择性去甲基化

    公开(公告)号：US3963760A

    公开(公告)日：1976-06-15

    申请号：US613423

    申请日：1975-09-15

    申请人： Luigi Bernardi ,  Bianca Patelli

    发明人： Luigi Bernardi ,  Bianca Patelli

    IPC分类号： C07C69/95 ,  C07C87/10

    CPC分类号： C07C69/95

    摘要： Anthracycline derivatives of the formula ##SPC1##Wherein R.sub.1, R.sub.2, R.sub. 3 and R.sub.4 are independently selected from the group consisting of hydrogen, chlorine, bromine and methoxy, with the proviso that at least one of the substituents is methoxy, and wherein R.sub.5 is selected from the group consisting of hydrogen, OH OR and OCOR; R being an alkyl group of 1 to 4 carbon atoms are prepared, in a single step, by selectively demethylating a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above by treating same with an aluminum halide in the presence of a suitable solvent at a temperature of 0.degree. to 50.degree.C.

    摘要翻译： 式WHEREIN R 1，R 2，R 3和R 4的蒽环类衍生物独立地选自氢，氯，溴和甲氧基，条件是至少一个取代基是甲氧基，其中R 5选自 由氢，OH OR和OCOR组成的组; 在一个步骤中，通过选择性地使下式化合物去甲基化制备R 1为1至4个碳原子的烷基：

    Ergoline derivatives and a process for their preparation
    9.
    发明授权
    Ergoline derivatives and a process for their preparation 失效
    艾尔莫林衍生物及其制备方法

    公开(公告)号：US4196288A

    公开(公告)日：1980-04-01

    申请号：US856536

    申请日：1977-12-01

    申请人： Enzo Beacco ,  Luigi Bernardi ,  Enrico Di Salle ,  Giovanni Falconi ,  Bianca Patelli

    发明人： Enzo Beacco ,  Luigi Bernardi ,  Enrico Di Salle ,  Giovanni Falconi ,  Bianca Patelli

    IPC分类号： A61K31/48 ,  A61K31/495 ,  A61K31/505 ,  C07D457/02

    CPC分类号： C07D457/02

    摘要： New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH.sub.2 and COOH.

    摘要翻译： 公开了新的麦角灵衍生物，其是具有以下结构的式（I）的化合物：其中R 1是氢或甲氧基; R2是氢或甲基; 并且X是羟基，R 3 COO，S-R 4或NR 5 R 6，其中R 3是具有1至6个碳原子的直链或支链烷基，未取代或取代的苯基，所述取代基选自氯，溴，烷基 或具有1至4个碳原子的烷氧基，含3至6个碳原子的环烷基或杂环; R 4是苯基或杂环，R 5和R 6是具有1至4个碳原子的烷基，或与它们相连的N原子一起形成杂环。 杂环可以是含有1至3个选自氮，氧和硫的杂原子的5或6元环，并且可以是饱和或不饱和的，未取代的或被卤素取代的烷基，具有1个 至3个碳原子，羟基，硝基，氨基，CONHNH 2和COOH。