Способ получения ненасыщенных производных 7-ациламидо-3-цефем-4-карбоновой кислоты или их сложных эфиров или их солей с щелочными металлами

Способ получения -метокси- -ХлОРМЕТилцЕфЕМОВ

Способ получения производных 7-(2-тиенил)-ацетамидо-7-метокси-3-пиразинилтиометил-3-цефем-4-карбоновой кислоты

Способ получения производных цефалоспорина

Способ получения производных 7-амино-цефалоспорановой кислоты

Способ получения кристаллической модификации натриевой соли 7 цианацетиламино-3-ацетоксиметил3-цефем-4-карбоновой кислоты

Способ получения производных 3-замещенных тиометилцефалоспоринов или их этиловых или дифенилметиловых эфиров или их солей

... 1. Способ получения производных 3-замещенных тиометилцефалоспоринов формулы RI S pJ--Nx -CHzS Ri-, СООН где R, - аминогруппа или группа формулы R3-CH N в которой R-5 - 2-оксифенш1 или 3,5-ди- трет-бутил-4-оксифенил; R2 - 1,2,3,4-тетразолш1-5, свободный или замещенный в положении 1 метилом, этилом, карбоксиметилом, карбамоилметилом, сульфометилом, 2оксиэтилом , 2-аминоэтилом или фенилом, 1,3,4-тиадиазолил-2, свободный или замещенный в положении 5 метилом, 1,2,3-триазолил-5, бензоксазолил-2,бензимидазолил-2, 2-метш1-2,5-ДИГИДРО-5-ОКСО-6-ОКСИ-ас-триазин-3-ип , пропил, фенил, карбоксиметил или этоксикарбонилметил или их этиловых ипи дифенилметиловых эфиров, или их солей взаимодействием соединения формулы X 1 снгосошз СООН где RI имеет указанные значения; (Л Y - радикал - S - или - S - или его соответствующего сложного эфира, или его соли с тиолом формулы R 2 - SH, где Rrt имеет указанные значения, или с его солью в среде органического растворителя при температуре от -20 до 80 С, отличаюсд щийся ...

Способ получения ненасыщенных производных 7-ациламидо-3-цефем4-карбоновой кислоты или их солей

VERFAHREN ZUR GEWINNUNG VON CEPHALOSPORIN C

METHOD OF CONVERTING CEPHALOSPORIN C TO A DERIVATIVE THEREOF

... 1324419 N-haloalkanoyl derivatives of cephalosporin C ELI LILLY & CO 12 Oct 1970 [17 Dec 1969] 48320/70 Heading C2A Cephalosporin C is converted to an N-haloalkanoyl derivative of formula wherein R is an -halo or ,-dihalo-C 2 -C 4 alkanoyl group, by acylating the amino group in the adipoyl side chain with a corresponding haloalkanoyl halide or anhydride. The cephalosporin C may be treated in aqueous solution, e.g. a productive fermentation broth which preferably has been filtered and if necessary concentrated, to convert it to the said derivative which is easily extracted from the aqueous medium with a water-immiscible solvent such as ethyl acetate. The acylating agent is preferably an -halo or ,-dihaloalkanoyl chloride or mixed anhydride (e.g. acetic chloroacetic anhydride). The solvent extraction is best conducted at acid pH and immiscible solvents used include propyl or butyl acetate, nitriles and ketones. Alkyl esters may be mixed with one tenth to one volume of C 2 to C 4 alkanol.

CEPHALOSPORIN DERIVATIVES

ALPHA-AMINOACYL-3-HALO-CEPHALOSPORINS

... 1461323 Silylated x-aminoacyl-3-halo-cephalosporins ELI LILLY & CO 22 Feb 1974 [23 Feb 1973] 8097/74 Heading C3P [Also in Division C2] Novel compounds of the Formula I wherein R is phenyl,mono- or dihydroxy phenyl, mono or dihalophenyl, mono or dimethylphenyl, mono- or dimethoxyphenyl, 2- or 3-thienyl or 2- furyl; R 1 is hydrogen, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, 2,2,2- trichloroethyl, trimethylsilyl or t-butyl; R 2 is hydrogen or an amino-protecting group; X is fluoro, chloro or bromo and pharmaceutically acceptable salts thereof when R 1 or R 2 is hydrogen, may be prepared by (i) halogenating and acylating in either order a compound of the Formula II wherein R 3 is a carboxylic acid protecting ester forming group optionally followed by removal of the carboxylic acid protecting ester forming group and or the amino-protecting group or (ii) fluorinating a 3-alkyl or aryl sulphonate of a compound II (R 1 #H) having a protected amino group, followed by acylation. In ...

CEPHALOSPORINS

... 1487369 Silylated cephalosporins E R SQUIBB & SONS Inc 9 Dec 1974 [28 Dec 1973 10 May 1974] 53116/74 Heading C3S [Also in Division C2] Novel compounds I (R 1 is H, 1-8C alkyl, phenyl or phenyl-1-8C alkyl-optionally substituted by halo, 1-8C alkyl or alkoxy, OH or COOH- or R 1 is 5-6- membered heterocyclyl optionally substituted by halo, 1-8C alkyl or alkoxy or phenyl; R 2 is 1-8C alkyl; R 3 is tri(1-8C alkyl)silyl and R 4 is H, acetoxy, a quaternary ammonium radical, 1-8C alkylthio, heterocyclylthio or a nitrogenlinked radical of an amine) are prepared by reaction of a compound II or an acylating derivative thereof with a compound III ...

PROCESS FOR THE RECOVERY OF CEPHALOSPORIN C AND DERIVATIVES THEREOF

... 1489231 Cephalosporin derivatives ALFA FARMACEUTICI SpA 22 Jan 1975 [20 Feb 1974] 7699/74 Heading C2C The invention comprises a process for the recovery of cephalosporin derivatives from aqueous mediums containing cephalosporin C or substituted cephalosporin C by treating said mediums with sulphonyl chlorides of the formula R.SO 2 Cl, wherein R is an optionally substituted C 4-10 alkyl or aryl radical, to convert the cephalosporin C or substituted cephalosporin C to the corresponding N-(alkyl sulphonyl)- cephalosporins or N-(arylsulphonyl)cephalosporins and extracting said N-(alkylsulphonyl)- cephalosporins or N - (arylsulphonyl)cephalosporins with water-immiscible solvents; a process for preparing 7-amino cephalosporanic acid from N-(alkylsulphonyl)cephalosporin C or salt thereof or N-(arylsulphonyl) cephalosporin C or salt thereof by protecting the carboxylic groups by formula of a diester, halogenating the diester to give the corresponding iminohalide; reacting the imino-halide with ...

CEPHALOSPORINS AND PROCESSES FOR PRODUCING SAME

PROCESS FOR PREPARATION OF CEPHALOSPORIN DERIVATIVES

CEPHALOSPORIN DERIVATIVES

... 1525687 Cephalosporins TAKEDA YAKUHIN KOGYO KK 31 March 1977 [2 April 1976] 13688/77 Heading C2C Novel therapeutic compounds (I) wherein X is hydrogen, hydroxyl, acyloxy, alkoxy, carbamoyloxy, quaternary ammonium, or a group of the formula -SR1 (where R1 is a nitrogen-containing heterocyclic group) or a pharmaceutically acceptable salt or ester thereof, are made by standard methods.

New derivatives of cephalosporines, their method of preparation and drugs antibiotic container the aforementioned derivatives

Method of preparation of cephalosporine-sul-fonates (esters).

Method of preparation of ethers d'& - aminoacylcéphalosporine.

Improvements relative to derivatives of naphtylglycyl-cephalosporines.

Method of preparation of a-aminoacyl-3-halocépha-losporines.

New crystalline form of the sodium salt of céphacétril and its method of preparation.

PROCEDURE FOR MANUFACTURING NEW DERIVATIVES of the 7-ACYLAMIDO-3-CEPHEM-4-CARBONSAEURE AND YOUR SALTS

PROCEDURE FOR THE PRODUCTION OF A MIXTURE OF NEW ANTIBIOTICS

PROCEDURE FOR THE PRODUCTION OF 3 (THIOMETHYL) CEPHALOSPORINEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN ALFA-AMINOACYLCEPHALOSPORINATHERN UND DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN ANTIBIOTISCHEN VERBINDUNGEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN CYANOMETHYLTHIOACETYLCEPHALOSPORINEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN CEPHALOS- PORINDERIVATEN

VERFAHREN ZUR GEWINNUNG VON CEPHALOSPORIN C, SEINEN SALZEN UND DERIVATEN AUS KULTURFILTRATEN ODER -LOESUNGEN

VERFAHREN ZUM HERSTELLEN DES ANTIBIOTIKUMS CEPHEMIMYCIN

VERFAHREN ZUR HERSTELLUNG VON CEPHALOSPORINEN

VERFAHREN ZUR HERSTELLUNG VON PENICILLIN- UND CEPHALOSPORINSAURE-DERIVATEN

VERFAHREN ZUR RUCKGEWINNUNG VON CEPHALOSPORIN C AUS WASSERIGEN MEDIEN IN FORM EINES SULFONAMIDS

VERFAHREN ZUR HERSTELLUNG VON NEUEN 7-ACYLAMIDO-3-CEPHEM-4-CARBONSAUREDERIVATEN

VERFAHREN ZUR HERSTELLUNG VON 7-ALKOXY-3- CHLORMETHYL-3-CEPHEMEN

PROCEDURE FOR THE PRODUCTION OF CEPHALOSPORANSAEURE ONES DERIVATIVES

PROCEDURE FOR the PRODUCTION OF 7-ACYLAMINO DESACETOXY CEPHALOSPORANSAURE ONE DERIVATIVES

PROCEDURE FOR the PRODUCTION of a 7-AMINOCEPHALOSPORIN-4-CARBONSAURE

PROCEDURE FOR MANUFACTURING NEW DERIVATIVES of the 7-ACYLAMIDO-3-CEPHEM-4-CARBONSAEURE AND YOUR SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 7-ACYLAMIDO-3-CEPHEM-4-CARBONSAUREDERIVATEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 6-ACYLAMIDO -3-CEPHEM-4 CARBON SOUR DERIVATIVES

PROCEDURE FOR the PRODUCTION OF NEW ONE 7-ACYLAMIDO-3-CEPHEM-4-CARBONSAUREDERIVATEN

PROCEDURE FOR the SELECTIVE ONE PROTECTION OR FOR the SELECTIVE ONE BLOCKING the GROUP OF CARBOXYLS of the 7-SEITENKETTE 7 - (4 ' - CARBOXYBUTANAMIDO) - CEPHALOSPORIN-4-CARBONSAURE

PROCEDURE FOR MANUFACTURING THE ANTIBIOTIC CEPHEMIMYCIN

PROCEDURES FOR THE PRODUCTION OF NEW CEPHALOS PORINDERIVATEN

PROCEDURE FOR the SELECTIVE ONE PROTECTION OR FOR the SELECTIVE ONE BLOCKING the GROUP OF CARBOXYLS of the 7-SEITENKETTE 7 - (4 ' - CARBOXYBUTANAMIDO) - CEPHALOSPORIN-4-CARBONSAURE

PROCEDURE FOR THE PRODUCTION OF CEPHALOSPORINDERIVATEN

ENZYMATIC PROCEDURE FOR THE PRODUCTION OF 7 AMINOCEPHALOSPORINSÄURE AND DERIVATIVES

3,7-DISUBSTITUIERTE-2 OR -3-CEPHEM-4CARBONS [URE CONNECTIONS, IT ABSTENTIONS PHARMACEUTICAL COMPOSITIONS AND PROCEDURES TO THEIR PRODUCTION.

PROCEDURE FOR THE PRODUCTION OF NEW CYANOMETHYLTHIOACETYLCEPHALOSPORINEN

PROCEDURE FOR the PRODUCTION of a 7BETA-ACYLAMIDO-3-METHYL-CEPH-3-EM-4-CARBONSAURE

Procedure for the extraction of Cephalosporin C-products

PROCEDURE FOR THE PRODUCTION OF NEW CEPHALOSPORINDERIVATEN

PROCEDURE FOR the PRODUCTION OF 7-ALFA-AMINOACETAMIDOCEPHALOSPORIN-4-CARBONSAUREN

VERFAHREN ZUM HERSTELLEN VON NEUEN HETEROMONO- CYCLISCHEN UND HETEROBICYCLISCHEN DERIVATEN UNGESAETTIGTER 7-ACYLAMIDO-3-CEPHEM-4-CARBON- SAEUREN, IHREN SALZEN UND ISOMREN

ANTIMICROBIAL CHINOLONYL LACTAMS

Procedure for the production of new N-Acylverbindungen of the 6-Aminopenicillansäure and the 7-Aminocephalosporansäure

BIOLOGICALLY ACTIVE CONNECTIONS OUT GANODERMA PFEIFFERI DMS 13239

TRIFLUOROMETHYLMERCAPTOACETAMIDOCEPHALOSPORINS

BETA-LACTAM COMPOUNDS

PENICILLINS AND CEPHALOSPORINS

CEPHALOSPORIN DERIVATIVES

NOVEL ANTIMICROBIAL FLUOROQUINOLONYL CEPHEMS

PREPARATION OF 3-HALOMETHYLCEPHEMS

The preparation of 7-acyl-3-(substituted carbamoyloxy)cephem compounds

Cephalosporin derivatives

CEPHALOSPORINS

CEPHAPIRINE ESTERS, SALTS THEREOF AND PROCESSES FOR PRODUCING THE SAME

UNSATURATED DERIVATIVES OF 7-ACYLAMIDO-3-CEPHEM-4- CARBOXYLIC ACID AND PROCESS FOR THEIR PREPARATION

This invention relates to compounds of the general formula I (I) wherein Z is cyano or carbamoyl; A is trans -CH=CH, cis -CH=CH or -C?C-; B is -O-?-CH3 or -S-Het wherein Het is one of the following groups , wherein R is hydrogen or methyl, or wherein R1 and R2 are independently selected from the group consisting of hydrogen and methyl; X is a free or esterified carboxy group, and pharmaceutically and veterinarily acceptable salts thereof. These compounds possess a high antibacterial activity against both Gram-positive and Gram-negative bacteria and are therefore useful in the treatment of infections caused by said microorganisms. This invention also provides a process for the preparation of these useful compounds.

7-((SUBSTITUTED-THIOMETHYL)-PHENYL) ACETAMIDOCEPHALOSPORIN DERIVATIVES

Novel compounds of the formula are useful as antibiotics.

ANTIMICROBIAL QUINOLONYL LACTAMS

ANTIMICROBIAL FLURORQUINOLONYL CEPHEMS

NOVEL ANTIMICROBIAL FLUOROQUINOLONYL CEPHEMS Thomas P. Demuth, Jr. Ronald E. White Antimicrobial fluoroquinolonyl cephems of the formula: wherein (1) R1 and R2 are groups among those known in the art for substitution at the 7-position of an antimicrobially-active cephem; (2) R3 is a substituted or unsubstituted, nitrogen-containing, heterocyclic moiety; and (3) R4 is hydrogen, halogen, lower alkoxy or cyclic alkoxy, amino, nitro or cyano. Preferably, R3 is substituted or unsubstituted piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R4 is preferably hydrogen or halogen.

PROCESS FOR PREPARING CEPHALOSPORINS

3-ARYLOXYMETHYL-CEPHALOSPORIN DERIVATIVES, THEIR PREPARATION AND THEIR MEDICAL USE

Compounds of formula (I): (I) ¢in which: R1 is hydrogen or acyl; R2 is hydrogen or C1 - C4 alkoxy; and Ar is phenyl or substituted phenyl! and pharmaceutically acceptable salts and esters thereof have valuable antibiotic activity, including against Methicillin-resistant strains of Staphylococcus. The invention also provides a process for preparing the compounds and methods and compositions using them.

CEPHALOSPORIN DERIVATIVES

NOVEL CEPHALOSPORIN DERIVATIVES of the disclosure A 2-(syn)-hydroxyimino-acetamide derivative of the formula; wherein Y is hydrogen, hydroxyl, an acyloxy, carbamoyloxy, a quaternary ammonium or a nitrogen-containing heterocyclic ring-substituted thio group; or pharmaceutieally acceptable salts or esters thereof are useful as antibacterial agent.

PENICILLINS AND CEPHALOSPORINS

CEPHAMYCINS

CEPHALOSPORINS AND PROCESS FOR THEIR PREPARATION

HETEROMONOCYCLIC AND HETEROBICYCLIC DERIVATIVES OF UNSATURATED 7-ACYLAMIDO-3-CEPHEM-4-CARBOXYLIC ACID AND PROCESS FOR THEIR PREPARATION

PROCESS FOR PRODUCING 7-(SUBSTITUED)AMINO -3-SUBSTITUTED THIOMETHYL-.DELTA.3-CEPHEM-4- CARBOXYLIC ACIDS

Verfahren zur Herstellung antimikrobiell wirksamer Verbindungen

Verfahren zur Gewinnung von schwerlöslichen Cephalosporin C-Komplexen

Verfahren zur Herstellung von 2-Cephemverbindungen

7-amino-cephalosporanic acid derivs with anti-bacterial - properties

Cpds. R1 = lower alkyl, R2 = H or lower alkoxycarbonyl R3 = OH, OH esterified by a carboxylic acid in which the O may be replaced by S, an optionally N-substd. carbamoyloxy group in which the O may be replaced by S, or a quaternary amino group, and salts (including internal salts) thereof. Antibacterials (Gram-positive, and -negative) active against, for example, penicillin-resistant Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Salmonella typhosa and Bacterium proteus. They can be used in the treatment of infections and as animal feed additives, as food preservatives, and disinfectants.

Verfahren zur Herstellung von 7-Aminocephalosporansäure (7-ACA) aus Cephalosporin C

VERFAHREN ZUR UMWANDLUNG VON CEPHALOSPORIN C ODER DESSEN CARBONSAEURESALZ IN EIN IN ORGANISCHEN LOESUNGSMITTELN LOESLICHES DERIVAT.