KARBONYLMETYL-DERIVAT

摘要

The invention comprises carbonylmethyl derivatives of the formula IA and corresponding carbonylmethylene derivatives of the formula IB (IA) (IB) in which R1a represents a member of the group comrising hydrogen and an acyl radical of the formula A Ra-C(Rb)(Rc)-C(=O)-(A) in which Ra represents a member of the group comprising optionally substituted phenyl, thienyl, furyl, cyclohexadienyl and cyclohexenyl, Rb represents hydrogen and Rc represents a member of the group comprising hydrogen, optionally protected hydroxyl, optionally protected amino and phenyl-lower protected sulpho, or in which Ra represents a member of the group comprising cyano, optionally substituted phenoxy, pyridylthio, and tetrazolyl, and Rb and Rc each represent hydrogen, or in which Ra represents a member of the group comprising phenyl, thienyl, furyl, and Rb and Rc together denote a member of the group comprising lower alkoxyimino, cycloalkoxyimino and phenyl-lower alkoxyimino in the syn-configuration, and such a group of the formula (A) contains at most one free amino group, R1b represents hydrogen, R2 represents a member of the group comprising hydroxyl, alpha -poly-branched lower alkoxy and 2-halogeno-lower alkoxy, which can easily be converted into the latter, and also phenacyloxy, 1-phenyl-lower alkoxy which has 1-3 phenyl radicals which are optionally substituted by lower alkoxy or nitro, lower alkanoyloxymethoxy, alpha -amino-lower alkanoyloxymethoxy, or 2-phthalidyloxy, and also tris-lower alkylsilyloxy, and R3 represents a member of the group comprising hydrogen, lower alkyl, cycloalkyl, phenyl which is optionally substituted by lower alkyl, lower alkoxy or halogen, phenyllower alkyl which is optionally substituted by nitro, lower alkyl, lower alkoxy or halogen, hydroxyl, etherified hydroxyl, especially lower alkoxy, above all methoxy, amino, lower alkylamino, di-lower alkylamino, lower alkyleneamino, oxa-lower alkylenamino, phenylamino, hydroxylamino, lower alkoxyamino, hydrazino, 2-lower alkylhydrazino, 2-phenylhydrazino, 4-lower alkylpiperazin-1-ylamino, lower alkylamino which is substituted by amino and/or carboxyl, and heterocyclylamino which is optionally substituted by lower alkyl, and wherein the heterocyclyl radical preferably contains 5-6 rings members and contains, as hetero-atoms, nitrogen, which is optionally also in the N-oxidized form, oxygen or sulphur and 1-oxides and salts of such compounds, which compounds are active against microorganisms, such as Gram-positive and Gram-negative bacteria, and pharmaceutical preparations containing these compounds.