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Bicyclo (3,2,1) octancarboxylsyrederivater and process for their preparation as well as the compounds' therapeutic use

机译:双环(3,2,1)正辛基羧基去干燥剂及其制备方法和化合物的治疗用途

摘要

1. Claims for the Contracting States BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Bicyclo (3.2.1.) octane-3-carboxylic acid derivatives, having the following general formula : see diagramm : EP0130882,P8,F2 in which : R represents a straight- or branched-chain lower alkyl radical Z represents a group OX in which X is hydrogen or an alkaline metal, or Z may also represent a group see diagramm : EP0130882,P8,F3 in which R1 and R2 , which may be the same or different, are hydrogen or a lower alkyl radical. 1. Claims for the Contracting State : AT Process for preparing Bicyclo (3.2.1.) octane-3-carboxylic acid derivatives, having the following general formula : see diagramm : EP0130882,P8,F4 in which : R represents a straight- or branched-chain lower alkyl radical Z represents a group OX in which X is hydrogen or an alkaline metal, or Z may also represent a group see diagramm : EP0130882,P8,F6 in which R1 and R2 , which may be the same or different, are hydrogen or a lower alkyl radical, comprising converting methyl 8-oxo-bicyclo (3.2.1.) octane-3-carboxylate having the formula : see diagramm : EP0130882,P8,F8 to an acid of the formula see diagramm : EP0130882,P9,F1 reacting the acid of the formula (III) with a strong base to give an intermediate organometallic compound having the formula see diagramm : EP0130882,P9,F2 in which B is an alkaline metal and, by action of an alkyl halide R-X in which R has the aforedisclosed meanings, converting compound (IV) to a compound of the formula (I) in which Z is OH, and preparing according to conventional methods the compounds of the formula (I) in which Z is other than OH.
机译:1.对缔约国的索赔BE,CH,DE,FR,GB,IT,LI,LU,NL,SE双环(3.2.1。)辛烷-3-羧酸衍生物,其通式如下:见图: EP0130882,P8,F2其中:R代表直链或支链低级烷基基团Z代表基团OX,其中X是氢或碱金属,或者Z也可以代表基团,见图:EP0130882,P8,F3其中R 1和R 2可以相同或不同,是氢或低级烷基。 1.缔约国的权利要求:AT制备具有以下通式的双环(3.2.1。)辛烷-3-羧酸衍生物的方法:参见示意图:EP0130882,P8,F4,其中:R代表直链或支链低级烷基基团Z代表一个基团OX,其中X是氢或碱金属,或者Z也可以代表一个基团,见图:EP0130882,P8,F6其中R1和R2可以相同或不同,烷氧基是氢或低级烷基,其包括将具有下式的八-氧代双环(3.2.1。)辛烷-3-羧酸甲酯转化为下式的酸:参见图EP0130882,P8,F8,参见图EP0130882, P9,F1,使式(Ⅲ)的酸与强碱反应,得到具有化学式的中间体有机金属化合物,参见图:EP0130882,P9,F2,其中B是碱金属,并通过卤代烷RX的作用其中R具有前述含义,将化合物(IV)转化为以下化合物式(I),其中Z为OH,并根据常规方法制备其中Z不是OH的式(I)化合物。

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