EFALOSPORINE, PROCEDIMENTO PER PRODURLE, AGENTI ANTIBATTERICI CHE LE CONTENGONO, INTERMEDI PER ESSE EPROCEDIMENTO PER PRODURRE GLI INTERMEDI

Cephalosporins of formula (I) and their salts are new. (R1 is H or carboxy-protecting gp.; R2 is a gp. (II)-(V); R6 is H, OH, NO2, (thio)carbamoyl or opt. substd. alkyl, alkynyl, alka(di)enyl, cycloalk(en)yl, cycloalkadienyl, ar(alk)yl, alkylthio, acyl(oxy), (cyclo)alkoxy, aryloxy, (cyclo)alkoxycarbonyl, acyloxycarbonyl, aralkoxycarbonyl, (cyclo)alkylsulphonyl, arylsulphonyl, heterocyclyl sulphonyl, mono- or di-alkyl-carbamoyl or thiocarbamoyl, acylcarbamoyl, acylthiocarbamoyl, alkylsulphonyl- or arylsulphonyl-carbamoyl or thiocarbamoyl, sulphamoyl (opt. mono or di-alkyl substd.), alkoxythiocarbonyl, alkylideneamino, cycloalkylmethyleneamino, arylmethyleneamino, heterocyclyl methyleneamino, heterocyclyl or NR16R17. R16 and R17 are H or alkyl, or together complete a ring; R7-12 and R14-15 are each H, halo or opt. substd. alkyl, aralkyl or aryl; R13 is H, halo, carboxy, sulpho, (thio)carbamoyl or substd. alkyl, ar(alk)yl, alkoxy, alkylthio, acyl, (cyclo)alkoxycarbonyl, acyloxycarbonyl, aralkoxycarbonyl, (cyclo)alkylsulphonyl, arylsulphonyl, heterocyclic sulphonyl, alkyl or dialkyl-carbamoyl or thiocarbamoyl, acyl(thio)carbamoyl, alkyl- or aryl-sulphonylcarbamoyl or sulphonylthiocarbamoyl; R3 is H or alkoxy; R4 is H or halo; R5 is H or opt. protected amino; A is methylene or :CN:N-OR18 (syn and/or anti); R18 is H, alk(en)yl, alkynyl, cycloalk(en)yl, ar(alk)yl, heterocyclyl (all opt. substd.), hydroxy-protecting gp. or a gp. -P(O)(R19)(R20). R19 and R20 are each OH, (ar)alkyl, aryl, (ar)alkoxy or aryloxy. (I) are antibacterials with a broad spectrum of activity, good stability against beta-lactamase; good resorption when given orally or parenterally, or low toxicity (LD50 at least 2 g/kg intravenously in mice).