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PROCESS FOR PREPARING 6-AMINO-PENICILLANIC ACID DERIVATIVES

机译:制备6-氨基-青霉酸衍生物的方法

摘要

1. Claims (for the Contracting States : CH, IT, LI, LU, NL, SE) A process for the manufacture of 6-aminopenicillanic acid derivatives of the general formula see diagramm : EP0049891,P5,F1 in which R represents hydrogen or a readily hydrolyzable ester group, as well as of pharmaceutically compatible salts of these compounds, characterized by hydrogenating a compound of the general formula see diagramm : EP0049891,P5,F2 in which R has the significance given above and R**1 signifies a hydrogenolytically cleavable group, or a salt of such a compound in the presence of palladium/carbon, whereafter, if desired, an ester of formula I obtained is subjected to an ester cleavage, if desired a carboxylic acid of formula I obtained is treated with an agent yielding the ester group R and, if desired, a compound of formula I obtained is converted into a pharmaceutically compatible salt thereof. 1. Claims (for the Contracting State : AT) A process for the manufacture of 6-aminopenicillanic acid derivatives of the general formula see diagramm : EP0049891,P5,F4 in which R represents hydrogen or a readily hydrolyzable ester group, as well as of pharmaceutically compatible salts of these compounds, characterized by hydrogenating a compound of the general formula see diagramm : EP0049891,P6,F1 in which R has the significance given above and R**1 signifies a hydrogenolytically cleavable group, or a salt of such a compound in the presence of palladium/carbon, whereafter, if desired, an ester of formula I obtained is subjected to an ester cleavage, if desired a carboxylic acid of formula I obtained is treated with an agent yielding the ester group R and, if desired, a compound of formula I obtained is converted into a pharmaceutically compatible salt thereof.
机译:1.权利要求(对于缔约国:CH,IT,LI,LU,NL,SE)一种通式为6的氨基青松酸衍生物的制备方法,参见示意图:EP0049891,P5,F1,其中R代表氢或易水解的酯基以及这些化合物的可药用盐,其特征在于将通式的化合物加氢,参见图表:EP0049891,P5,F2,其中R具有上述意义,R ** 1表示氢解可裂解基团,或在钯/碳存在下的此类化合物的盐,此后,如果需要,将得到的式I的酯进行酯裂解,如果需要,用试剂处理得到的式I的羧酸产生酯基R,并且如果需要,将获得的式I化合物转化为其可药用盐。 1.权利要求(对于缔约国:AT)一种通式为6-氨基青松酸衍生物的制备方法,参见图:EP0049891,P5,F4,其中R代表氢或易于水解的酯基,以及这些化合物的药学上相容的盐,其特征在于将通式的化合物氢化,见图:EP0049891,P6,F1,其中R具有上述含义,R ** 1表示可氢解的基团,或此类化合物的盐在钯/碳存在下,此后,如果需要,将获得的式I的酯进行酯裂解,如果需要,将获得的式I的羧酸用产生酯基R的试剂处理,并且如果需要,将获得的式I化合物转化为其可药用盐。

著录项

  • 公开/公告号PT73822B

    专利类型

  • 公开/公告日1983-11-07

    原文格式PDF

  • 申请/专利权人 F HOFFMANN LA ROCHE & CIE SA;

    申请/专利号PT19810073822

  • 发明设计人 ANDRE FURLENMEIER;

    申请日1981-10-14

  • 分类号C07D499/04;C07D499/78;

  • 国家 PT

  • 入库时间 2022-08-22 11:01:57

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