首页> 外国专利> Method of preparation of isomers synthesis of compounds of acids (3,7 - cephem - 4 - carboxylic 3,7 - disubstituted and novel products thus obtained, for anti-bacterial effect

Method of preparation of isomers synthesis of compounds of acids (3,7 - cephem - 4 - carboxylic 3,7 - disubstituted and novel products thus obtained, for anti-bacterial effect

机译:异构体的制备方法合成酸(3,7-头孢烯-4-羧酸3,7-双取代的化合物)及由此获得的新产品,具有抗菌作用

摘要

Novel syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds are provided of the formula: IMG in which R1 is a group of the formula: IMG wherein R5 is hydrogen, halogen, nitro, hydroxy, lower alkoxy or acyloxy and R6 is hydroxy, lower alkoxy, acyloxy, acylamino or di(lower)alkylamino; a group of the formula: IMG wherein R7 is amino, protected amino, hydroxy or lower alkyl; or a group of the formula: IMG wherein R8 is lower alkyl and R9 is imino, protected imino or oxo; R2 is an aliphatic hydrocarbon group which may have suitable substituent (s); R3 is carboxy or protected carboxy; and R4 is acyloxymethyl, hydroxymethyl, formyl or a heterocyclicthiomethyl group which may have suitable substituent (s); or R3 and R4 are linked together to form -COOCH2-, and pharmaceutically acceptable salts and tautomers thereof; the novel compounds are highly active against a number of pathogenic bacteria.
机译:提供了具有以下化学式的3,7-二取代的3-cephem-4-羧酸化合物的新型同分异构体:其中R 1为具有化学式的基团:其中IM 5为氢,卤素,硝基,羟基,低级烷氧基或酰氧基,R 6是羟基,低级烷氧基,酰氧基,酰氨基或二(低级)烷基氨基;式:IMG,其中R7是氨基,被保护的氨基,羟基或低级烷基;或下式的基团:其中R 8为低级烷基且R 9为亚氨基,被保护的亚氨基或氧代;或R 2是可以具有合适的取代基的脂族烃基; R3是羧基或被保护的羧基; R4是可以具有适当取代基的酰氧基甲基,羟甲基,甲酰基或杂环硫代甲基; R3和R4连接在一起形成-COOCH2-及其药学上可接受的盐和互变异构体;该新型化合物对许多病原菌具有高活性。

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