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Process for the preparation of 6-aminopenicillanic

2024-09-09 来源:化拓教育网
专利内容由知识产权出版社提供

专利名称:Process for the preparation of 6-aminopenicillanic-acid derivatives, andintermediates therefor

发明人:FURLENMEIER, ANDRE, DR.申请号:EP81108244.5申请日:19811012公开号:EP0049891A1公开日:19820421

摘要:1. Claims (for the Contracting States : CH, IT, LI, LU, NL, SE) A process for themanufacture 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 byhydrogenating a compound of the general formula see diagramm : EP0049891,P5,F2 inwhich R has the significance given above and R**1 signifies a hydrogenolytically cleavablegroup, or a salt of such a compound in the presence of palladium/carbon, whereafter, ifdesired, an ester of formula I obtained is subjected to an ester cleavage, if desired acarboxylic acid of formula I obtained is treated with an agent yielding the ester group Rand, if desired, a compound of formula I obtained is converted into a pharmaceuticallycompatible salt thereof. 1. Claims (for the Contracting State : AT) A process for themanufacture 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 byhydrogenating 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 cleavablegroup, or a salt of such a compound in the presence of palladium/carbon, whereafter, ifdesired, an ester of formula I obtained is subjected to an ester cleavage, if desired acarboxylic acid of formula I obtained is treated with an agent yielding the ester group Rand, if desired, a compound of formula I obtained is converted into a pharmaceuticallycompatible salt thereof.

申请人:F. HOFFMANN-LA ROCHE & CO. AKTIENGESELLSCHAFT

地址:Postfach 3255 4002 Basel CH

国籍:CH

代理机构:Lederer, Franz, Dr.

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