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    Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof as the use thereof as cytostatics
    3.
    发明授权
    Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof as the use thereof as cytostatics 失效
    半合成非对映异构体纯的N-缩水甘油环内酯，其作为细胞抑制剂的用途的立体选择性制备方法

    公开(公告)号：US5602108A

    公开(公告)日：1997-02-11

    申请号：US464468

    申请日：1995-06-05

    申请人： Manfred Gerken ,  Monika Grimm ,  Ernst Raab ,  Dieter Hoffmann ,  Reiner Straub

    发明人： Manfred Gerken ,  Monika Grimm ,  Ernst Raab ,  Dieter Hoffmann ,  Reiner Straub

    IPC分类号： A61K31/65 ,  A61K31/70 ,  A61K31/704 ,  A61P35/00 ,  C07B53/00 ,  C07C15/62 ,  C07C50/36 ,  C07H15/252 ,  C07H15/26 ,  A61K37/00 ,  C07M15/24

    CPC分类号： C07H15/26 ,  C07H15/252

    摘要： Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof and the use thereof as cytostatics. The invention relates to anthracyclines having cytostatic activity and the formula I, which are, where appropriate, in the form of a salt with an inorganic or organic acid, ##STR1## in which R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen, a hydroxyl group or an alkyloxy group (C.sub.1 -C.sub.4),R.sup.3 is hydrogen, a hydroxyl group or a structure of the formula II ##STR2## R.sup.4 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH,R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II,R.sup.6 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group, a tetrahydropyranyl group,R.sup.7 is hydrogen, an alkyl group (C.sub.1 -C.sub.4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group andR.sup.8 is a structure of the formula III or IV ##STR3## and to a process for the preparation of these compounds, which comprises reacting an anthracycline derivative of the structure I in whichR.sup.1, R.sup.2 and R.sup.4 are as defined above, andR.sup.3 is hydrogen, a hydroxyl group or a structure of the formula V ##STR4## R.sup.5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula V andR.sup.6 and R.sup.7 are as defined above, with (R)- or (S)-glycidyl sulfonate.

    摘要翻译： 半合成非对映体纯N-缩水甘油环素，其立体选择性制备方法及其作为细胞抑制剂的用途。 本发明涉及具有细胞抑制活性的蒽环类抗生素和式I，它们在适当的情况下为无机或有机酸形式的盐，其中R 1为氢或羟基，R 2为氢， 羟基或烷氧基（C 1 -C 4），R 3是氢，羟基或式II的结构。R 4是CH 2 CH 3，COCH 3，COCH 2 OH，CHOHCH 3或CHOHCH 2 OH，R 5是氢，羟基 ，甲氧基羰基或式II的结构，R6是氢，烷基（C1-C4），烯丙基，苄基或单 - 或二 - 甲氧基取代的苄基，四氢吡喃基，R7是 氢，烷基（C1-C4），烯丙基，苄基或单 - 或二 - 甲氧基取代的苄基，R8是式III或IV的结构，IV和 一种制备这些化合物的方法，其包括使结构I的蒽环衍生物与其中R 1，R 2和/ R 4如上定义，并且R 3是氢，羟基或式V R 5的结构是氢，羟基，甲氧基羰基或式V和R 6和R 7的结构如上定义 （R） - 或（S） - 磺酰基磺酰基。

    Electrophotographic photoconductor, pyrene-ring-containing olefin compound for use in the same, intermediate for synthesizing the olefin compound, and method of synthesizing the olefin compound
    4.
    发明授权
    Electrophotographic photoconductor, pyrene-ring-containing olefin compound for use in the same, intermediate for synthesizing the olefin compound, and method of synthesizing the olefin compound 失效
    用于其的电子照相感光体，含芘环的烯烃化合物，用于合成烯烃化合物的中间体以及合成烯烃化合物的方法

    公开(公告)号：US5569800A

    公开(公告)日：1996-10-29

    申请号：US433714

    申请日：1995-05-02

    申请人： Tamotsu Aruga ,  Masaomi Sasaki ,  Tomoyuki Shimada ,  Hiroshi Adachi

    发明人： Tamotsu Aruga ,  Masaomi Sasaki ,  Tomoyuki Shimada ,  Hiroshi Adachi

    IPC分类号： C07C15/62 ,  C07C25/24 ,  C07D209/86 ,  C07F9/40 ,  C07C1/32 ,  C07C15/38

    CPC分类号： C07D209/86 ,  C07C15/62 ,  C07C25/24 ,  C07F9/4056 ,  C07C2103/50

    摘要： An electrophotographic photoconductor which is composed of an electroconductive support and a photoconductive layer formed thereon comprising a novel pyrene-ring-containing olefin compound having formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or an alkyl group which may have a substituent; Y is an aliphatic hydrocarbon group which may have a substituent, a cyclic hydrocarbon group which may have a substituent, or an aromatic group which may have a substituent; n is an integer of 0 or 1, and m is an integer of 1 to 3, provided that when n is 0, m is 1, R.sup.1 is hydrogen, and Y is an aromatic group with a substituent ##STR2## R.sup.2 and R.sup.3 each represent hydrogen, and Y and R.sup.1 may be bonded to form a ring, a method of synthesizing the pyrene-ring-containing olefin compound and an intermediate therefor are disclosed.

    摘要翻译： 由导电载体和形成在其上的光电导层组成的电子照相感光体包含具有式[I]的新的含芘环的烯烃化合物：其中R1和R2各自表示氢或烷基， 可以具有取代基; Y是可以具有取代基的脂族烃基，可以具有取代基的环状烃基或可以具有取代基的芳香族基; n为0或1的整数，m为1〜3的整数，条件是当n为0时，m为1，R 1为氢，Y为具有取代基的芳基R2和R3 代表氢，Y和R 1可以键合形成环，公开了合成含芘环的烯烃化合物及其中间体的方法。

    Electrophotographic photoconductor with pyrene-ring-containing olefin compound for use in the same
    8.
    发明授权
    Electrophotographic photoconductor with pyrene-ring-containing olefin compound for use in the same 失效
    具有芘环的烯烃化合物的电子照相感光体用于其中

    公开(公告)号：US5268246A

    公开(公告)日：1993-12-07

    申请号：US682324

    申请日：1991-04-09

    申请人： Tamotsu Aruga ,  Masaomi Sasaki ,  Tomoyuki Shimada ,  Hiroshi Adachi

    发明人： Tamotsu Aruga ,  Masaomi Sasaki ,  Tomoyuki Shimada ,  Hiroshi Adachi

    IPC分类号： C07C15/62 ,  C07C25/24 ,  C07D209/86 ,  C07F9/40 ,  G03G5/047

    CPC分类号： C07C15/62 ,  C07C25/24 ,  C07D209/86 ,  C07F9/4056 ,  C07C2103/50

    摘要： An electrophotographic photoconductor is composed of an electroconductive support and a photoconductive layer formed thereon comprising a novel pyrene-ring-containing olefin compound having formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or an alkyl group which may have a substituent; Y is an aliphatic hydrocarbon group which may have a substituent, a cyclic hydrocarbon group which may have a substituent, or an aromatic group which may have a substituent; n is an integer of 0 or 1, and m is an integer of 1 to 3, provided that when n is 0, m is 1, R.sup.1 is hydrogen, and Y is an aromatic group with a substituent ##STR2## R.sup.5 and R.sup.3 each represent hydrogen, and Y and R.sup.1 may be bonded to form a ring, a method of synthesizing the pyrene-ring-containing olefin compound and an intermediate therefor are disclosed.

    摘要翻译： 电子照相感光体由导电载体和形成在其上的光电导层组成，包含具有式[I]的新的含芘环的烯烃化合物：其中R 1和R 2各自表示氢或烷基， 具有取代基; Y是可以具有取代基的脂族烃基，可以具有取代基的环状烃基或可以具有取代基的芳香族基; n为0或1的整数，m为1〜3的整数，条件是当n为0时，m为1，R 1为氢，Y为具有取代基的芳基，R 5和R 3为 代表氢，Y和R 1可以键合形成环，公开了合成含芘环的烯烃化合物及其中间体的方法。