Process for preparing 1,4-bridged cyclohexane carboxylic acid derivatives
    6.
    发明授权
    Process for preparing 1,4-bridged cyclohexane carboxylic acid derivatives 失效
    制备1,4-桥环己烷羧酸衍生物的方法

    公开(公告)号:US5008409A

    公开(公告)日:1991-04-16

    申请号:US447513

    申请日:1989-12-07

    IPC分类号: C07C303/40 C07C311/20

    CPC分类号: C07C303/40

    摘要: A process for preparing a compound of Formula (I): ##STR1## wherein R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen or lower alkyl; Y is unsubstituted or substituted methylene, ethylene, vinylene or oxygen; m is 0 or 1; n is 0, 1 or 2; and q is 1, 2, 3 or 4; with the limitation that when m is 0, n is not 0, and when m is 1, n is not 2, which process comprises:(a) reacting an aldehyde of Formula (II); ##STR2## wherein R, Y, m and n are as defined above, under reaction conditions for the Wittig Reaction with a ylide of Formula (III):(R.sup.1).sub.3 P.dbd.CH(CH.sub.2).sub.q COOM (III) wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl or aryl, M is an alkali metal and q is as defined above;(b) treating the reaction mixture of step (a) with an alkaline earth metal halide under alkaline conditions to form the alkaline earth metal salt of the carboxylic acid of Formula (I);(c) extracting the alkaline earth metal salt of the carboxylic acid of Formula (I) in an organic solvent; and(d) recovering the free carboxylic acid of Formula (I) from the organic solvent.

    Preparation of 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives
    8.
    发明授权
    Preparation of 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives 失效
    2,3-反式-1,4-桥联环己烷磺酰胺衍生物的制备

    公开(公告)号:US5120865A

    公开(公告)日:1992-06-09

    申请号:US711562

    申请日:1991-08-30

    IPC分类号: C07C303/40 C07C311/20

    CPC分类号: C07C303/40 C07C2102/42

    摘要: A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.

    Pyrrolidine derivatives having phospholipase A.sub.2  inhibitory activity
    10.
    发明授权
    Pyrrolidine derivatives having phospholipase A.sub.2 inhibitory activity 失效
    具有磷脂酶A2抑制活性的吡咯烷衍生物

    公开(公告)号:US6147100A

    公开(公告)日:2000-11-14

    申请号:US355008

    申请日:1999-07-22

    摘要: A compound represented by the formula (I): ##STR1## wherein, for example, R.sup.1 is optionally substituted aralkyl, Z is nitrogen atom which optionally substituted with alkyl, X.sup.1 is --CH.sub.2 NHCO--, X.sup.2 is phenylene, X.sup.3 is a bond, Y.sup.2 is optionally substituted aryl, B is oxygen atom, its pharmaceutically acceptable salt, or hydrate thereof and a pharmaceutical composition which contains them as an active ingredient.

    摘要翻译: PCT No.PCT / JP98 / 00307 Sec。 371日期:1999年7月22日 102(e)日期1999年7月22日PCT提交1998年1月27日PCT公布。 公开号WO98 / 33797 日期:1998年6月8日由式(I)表示的化合物:其中,例如,R 1为任选取代的芳烷基,Z为任选被烷基取代的氮原子,X 1为-CH 2 NHCO-,X 2为亚苯基,X 3为键 ,Y2为任选取代的芳基,B为氧原子,其药学上可接受的盐或水合物,以及含有它们作为活性成分的药物组合物。