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7-(2-ARYL-2-(ETHERIFIED OXIMINO)ACETAMIDO)-3-(CARBAMOYLOXYYMETHYL)-CEPH-3-EM-4-CARBOXYLIC ACIDS AND THEIR DERIVATIVES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
7-(2-ARYL-2-(ETHERIFIED OXIMINO)ACETAMIDO)-3-(CARBAMOYLOXYYMETHYL)-CEPH-3-EM-4-CARBOXYLIC ACIDS AND THEIR DERIVATIVES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
Preparation of the syn isomer or of a mixture of syn isomer and anti isomer, where the content of the syn isomer is at least 90%, of 7-acylaminoceph-3-em-4-carboxylic acids with antibiotic activity and the formula I IMAGE in which B is S or S-O; R1 is furyl, thienyl or phenyl; and R2 is C1-C4-alkyl, C3-C7-cycloalkyl or phenyl, and of their non-toxic salts, including their solvates, and esters by acylation of the corresponding 7-amino compound, where appropriate with intermediate protection of the 4-carboxyl group and/or of the 3-carbamoyloxymethyl group, and subsequent isomerisation of a ceph-2-em compound which is obtained where appropriate to the ceph-3-em compound. The compounds are distinguished by a broad spectrum of action on pathogenic microorganisms, the ability to resist beta -lactamases and good stability in vivo.
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机译:顺式异构体或顺式异构体与反式异构体的混合物的制备,其中该顺式异构体的含量至少为90%,具有抗菌活性,且式I <7的7-酰基氨基ceph-3-em-4-羧酸IMAGE>,其中B是> S或> S-> O; R 1为呋喃基,噻吩基或苯基; R 2是C 1 -C 4烷基,C 3 -C 7环烷基或苯基,以及它们的无毒盐,包括它们的溶剂化物,和通过将相应的7-氨基化合物酰化而得到的酯,在适当的情况下具有中间保护基。 4-羧基和/或3-氨基甲酰氧基甲基,以及随后的ceph-2-em化合物的异构化,所述ceph-2-em化合物适合于ceph-3-em化合物。这些化合物的特点是对病原微生物具有广泛的作用,抵抗β-内酰胺酶的能力以及体内的良好稳定性。
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