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79 条记录 (耗时 0.021 秒)

    Method for the preparation of 9-amino camptothecin
    11.
    发明授权
    Method for the preparation of 9-amino camptothecin 失效
    9-氨基喜树碱的制备方法

    公开(公告)号：US5840899A

    公开(公告)日：1998-11-24

    申请号：US602792

    申请日：1996-09-30

    申请人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Franco Zarini

    发明人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Franco Zarini

    IPC分类号： C07D491/22

    CPC分类号： C07D491/22

    摘要： 9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.

    摘要翻译： PCT No.PCT / EP95 / 01692 Sec。 371日期1996年9月30日 102（e）1996年9月30日PCT PCT 1995年5月4日PCT公布。 公开号WO95 / 32207 PCT （I）的氨基喜树碱的制备通过以下方法制备：1）还原式（II）的化合物：其中Hal是10-或12-卤素 （I）的9-氨基喜树碱的单步骤，或者替代地，2a）从式（II）化合物还原性除去Hal基团，从而得到式（III）的化合物： III）和2b）还原式（III）的化合物，从而获得式（I）的9-氨基喜树碱; 所述步骤1和2a）和任选的步骤2b）各自在催化量的式PdL 2化合物的存在下进行，其中L是乙酸酯或卤素，另外在甲酸铵存在下，作为 氢源。 式（I）的9-氨基喜树碱可用作拓扑异构酶I的抑制剂。它可用于治疗癌症，特别是白血病，结肠和直肠肿瘤。

    (1'R,3S,4R)4-acylthio azetidinones
    14.
    发明授权
    (1'R,3S,4R)4-acylthio azetidinones 失效
    （1'R，3S，4R）4-酰硫基氮杂环丁酮

    公开(公告)号：US5399679A

    公开(公告)日：1995-03-21

    申请号：US54233

    申请日：1993-04-30

    申请人： Walter Cabri ,  Ilaria Candiani ,  Franco Zarini ,  Angelo Bedeschi

    发明人： Walter Cabri ,  Ilaria Candiani ,  Franco Zarini ,  Angelo Bedeschi

    IPC分类号： C07D205/09 ,  C07D401/12 ,  C07D405/12 ,  C07D499/88 ,  C07D499/897 ,  C07F7/18 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D401/12 ,  C07D205/09 ,  C07D405/12 ,  C07D499/88 ,  C07F7/186 ,  Y02P20/55

    摘要： There is provided a process for preparing a compound of formula (I) ##STR1## wherein R is H or a hydroxy protecting group, R.sub.2 is an organic residue and R.sub.3 is H or a nitrogen protecting group, which process comprises reacting together a compound of formula (II) ##STR2## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl or a phenyl group, R and R.sub.3 are as defined above, a compound of formula (III) ##STR3## wherein R.sub.2 is as defined above and X is a cation or a silicon-containing residue, and a salt of a group IIa, IIb or transition element. The compounds of formula (I) are intermediates in the synthesis of penem antibiotics.

    摘要翻译： 提供了制备式（I）化合物的方法，其中R是H或羟基保护基，R 2是有机残基，R 3是H或氮保护基，该方法包括使 式（II）化合物其中R1是C1-C4烷基或苯基，R和R3如上所定义，式（III）化合物其中R 2是 如上所定义，X是阳离子或含硅残基，以及Ⅱa，Ⅱb族或过渡元素的盐。 式（I）化合物是合成penin抗生素的中间体。

    Process for the synthesis of exomethylenecephams
    15.
    发明授权
    Process for the synthesis of exomethylenecephams 失效
    合成异亚甲基脑炎的方法

    公开(公告)号：US5304641A

    公开(公告)日：1994-04-19

    申请号：US21174

    申请日：1993-02-16

    申请人： Walter Cabri ,  Ilaria Candiani ,  Angelo Bedeschi

    发明人： Walter Cabri ,  Ilaria Candiani ,  Angelo Bedeschi

    IPC分类号： B01J31/04 ,  B01J31/22 ,  C07B61/00 ,  C07D501/00 ,  C07D501/04 ,  C07D501/14 ,  C07D501/24 ,  C07D501/02

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： The present invention relates to a process for the preparation of exomethylene cephams, which are useful intermediates in the production of many useful .beta.-lactam antibiotics.More particularly there is provided a process for preparing a compound of formula I ##STR1## wherein n is O or 1, R.sub.1 is hydrogen atom or an organic residue and R.sub.2 is a carboxy protecting group, which process comprises reacting a compound of the formula II ##STR2## wherein X is halogen atom or acetoxy group and R.sub.1 n and R.sub.2 are as defined above with a lanthanide complex.

    摘要翻译： 本发明涉及一种制备二亚甲基cephams的方法，其是生产许多有用（β-）内酰胺抗生素的有用的中间体。 更具体地，提供了制备式I化合物（*化学结构*）I的方法，其中n为0或1，R 1为氢原子或有机残基且R 2为羧基保护基，该方法包括使化合物 式II（*化学结构*）II其中X为卤素原子或乙酰氧基，R 1 n和R 2如上所述与镧系元素络合物一起使用。

    Process for preparing anthracyclinones
    16.
    发明授权
    Process for preparing anthracyclinones 失效
    制备蒽醌的方法

    公开(公告)号：US5180758A

    公开(公告)日：1993-01-19

    申请号：US743373

    申请日：1991-08-26

    申请人： Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Franco Francalanci

    发明人： Walter Cabri ,  Ilaria Candiani ,  Silvia De Bernardinis ,  Franco Francalanci

    IPC分类号： B01J27/128 ,  B01J31/12 ,  C07B61/00 ,  C07C46/00 ,  C07C49/423 ,  C07C49/727 ,  C07C50/36 ,  C07C50/38

    CPC分类号： C07C46/00 ,  Y02P20/55

    摘要： 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.m wherein M represents a transition metal atom, L and L', which may be the same or different, each represent an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII): ##STR3## wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R.sub.1 OH wherein R.sub.1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR.sub.1 group; and(ii) introducing an .alpha.-hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII).

    Process for preparing penems
    19.
    发明授权
    Process for preparing penems 失效
    制作青铜器的过程

    公开(公告)号：US5621096A

    公开(公告)日：1997-04-15

    申请号：US558209

    申请日：1995-11-16

    申请人： Walter Cabri ,  Angelo Bedeschi

    发明人： Walter Cabri ,  Angelo Bedeschi

    IPC分类号： C07D499/08 ,  C07D499/861 ,  C12P37/00 ,  C12R1/685 ,  C12R1/72 ,  C12R1/80 ,  C07D499/00

    CPC分类号： C12P37/00

    摘要： The invention provides a process for the preparation of the compound of formula I ##STR1## wherein R is carboxy group or a carboxylate anion, by enzymatic hydrolysis with a lipase or an acylase in an alcoholic solution, of a compound of the formula II ##STR2## wherein R.sub.1, represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and R.sub.2 is a hydrogen atom, an alkyl, alkenyl, phcnyl, phenylalkyl or phenylalkenyl group having from 1 to 18 carbon atoms or an alkoxy group.

    摘要翻译： 本发明提供了一种制备式I化合物的方法，其中R是羧基或羧酸根阴离子，通过在醇溶液中通过酶水解与式Ⅱ化合物的醇溶液， 图像II其中R1表示氢原子或C1-C6烷基，R2是氢原子，具有1至18个碳原子的烷基，烯基，苯基，苯基或烷氧基。

    Crystalline teglicar
    20.
    发明授权
    Crystalline teglicar 失效
    结晶晶格

    公开(公告)号：US08598384B2

    公开(公告)日：2013-12-03

    申请号：US12672099

    申请日：2008-07-31

    申请人： Walter Cabri ,  Mauro Marzi ,  Fabrizio Giorgi ,  Emanuela Tassoni

    发明人： Walter Cabri ,  Mauro Marzi ,  Fabrizio Giorgi ,  Emanuela Tassoni

    IPC分类号： C07C229/00 ,  A01N33/02

    CPC分类号： C07C275/16

    摘要： The present invention relates to a new crystalline form of R-4-trimethylammonium-3-(tetradecylcarbamoyl)-amino butyrate (also named crystalline Form I of ST 1326 or teglicar), a process for its preparation and pharmaceutical compositions containing same.

    摘要翻译： 本发明涉及一种新的结晶形式的R-4-三甲基铵-3-（十四烷基氨基甲酰基） - 氨基丁酸酯（也称为ST1326的晶体形式I或晶体），其制备方法和含有它的药物组合物。