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13 条记录 (耗时 0.038 秒)

    Novel processes for the synthesis of certain bicyclo(4.2.0)octane derivatives with valuable therapeutic properties
    5.
    发明授权
    Novel processes for the synthesis of certain bicyclo(4.2.0)octane derivatives with valuable therapeutic properties 失效
    用于合成具有有价值的治疗性质的某些双环（4.2.0）辛烷衍生物的新方法

    公开(公告)号：US4927963A

    公开(公告)日：1990-05-22

    申请号：US346425

    申请日：1989-04-28

    申请人： Keith A. M. Walker ,  Denis J. Kertesz

    发明人： Keith A. M. Walker ,  Denis J. Kertesz

    IPC分类号： C07C59/46 ,  C07C59/62

    CPC分类号： C07C59/46 ,  C07C59/62

    摘要： A process for preparing compounds represented by the formula ##STR1## wherein: X is hydrogen or lower alkoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl, ##STR2## --(CH.sub.2).sub.m -phenyl or --CH.sub.2 O-phenyl; in which any phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, anda is an integer of 0, 1 or 2;b is an integer of 3-7;m is an integer of 0, 1 or 2,as a mixture or separately in a sequence starting from an epoxide represented by the formula ##STR3## and processes for making the novel intermediates.

    摘要翻译： 一种制备式（I）表示的化合物的方法，其中：X为氢或低级烷氧基; Y是氢，外 - （低级烷基）或内 - （低级烷基）; n是2-4的整数; R2是氢或甲基; 并且R 3是直链或支链烷基， - （CH 2）m - 苯基或-CH 2 O-苯基; 其中任何苯基可以任选被低级烷基，低级烷氧基，三氟甲基或卤素取代，和a是0,1或2的整数; b是3-7的整数; m为0或1或2的整数，作为混合物，或以由式（7）表示的环氧化物开始的顺序分开，以及制备新型中间体的方法。

    Process for preparing 1,3-dioxolane derivatives
    6.
    发明授权
    Process for preparing 1,3-dioxolane derivatives 失效
    1,3-二氧戊环衍生物的制备方法

    公开(公告)号：US5208331A

    公开(公告)日：1993-05-04

    申请号：US900568

    申请日：1992-06-18

    申请人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    发明人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    IPC分类号： C07D233/60 ,  C07D405/06 ,  C07D521/00

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.

    摘要翻译： 本发明提供了制备式（I）化合物的改进方法：其中：n为0,1或2; 每个R 1独立地为卤素或低级烷基; R2是硝基或-N（R3）R4，其中R3是氢或低级烷基; R4是氢，低级烷基，低级烷基磺酰基或-C（Y）R5，其中Y是氧或硫，R5是氢，低级烷基，低级烷氧基或-N（R6）R7，其中R6是氢或低级烷基，R7是氢 ，低级烷基或低级烷氧基羰基; 或R 3和R 4与N一起为吡咯烷子基，哌啶子基，吗啉代，硫代吗啉代或哌嗪子基，其中哌嗪基在4-位被-C（O）R 8任选取代，其中R 8是氢，低级烷基，低级烷氧基或氨基; 或其药学上可接受的盐。 这些化合物可用于治疗以高胆固醇血症为特征的疾病状态。

    Process for preparing 1,3-dioxolane derivatives
    10.
    发明授权
    Process for preparing 1,3-dioxolane derivatives 失效

    公开(公告)号：US5274108A

    公开(公告)日：1993-12-28

    申请号：US993789

    申请日：1992-12-21

    申请人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    发明人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    IPC分类号： C07D521/00 ,  C07D405/00 ,  C07D405/14

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.