NOVEL CEPHALOSPORIN AND SALT THEREOF

• Main Authors: YOSHIDA CHOSAKU, TANAKA KIYOSHI, WATANABE YASUO, KOMATSU MIWAKO, KISHIMOTO SUMIKO, TAI MASARU, SAIKAWA ISAMU, SANTO TETSUO
• Format: Patent
• Language: English
• Published: 10.01.1987
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

NEW MATERIAL:A compound expressed by formula I [R is H or protecting group of carboxyl group; R is substituted 1,3-thiazol-4-yl; R is (substituted) lower alkyl, lower alkenyl, lower alkynyl, aryl, cycloalkyl, aralkyl, acyl or heterocyclic ring-lower alkyl; R is (protected) amino; n is 0 or 1] and a salt thereof. EXAMPLE:Diphenylmethyl 3-(2-acetylaminothiazol-4-yl)-7-[2-(Z)-methoxyimino-2-(2- tritylaminothiazol-4-yl)acetamido]-3-cephem-4-carboxylate. USE:An antimicrobial agent (effective also against cephalosporin-resistant germs). PREPARATION:A compound expressed by formula II (R is H or lower alkyl; R is phenylacetyl, phenoxyacetyl or R ) as a starting material is halogenated cyclized, quaternized, oxidized, reduced and deacetylated according to reaction formulas and passed through reaction with a compound expressed by formula XIV to afford the aimed compound expressed by formula Ia.