Abstract: A method for the acylation of the 7-amino group of the cephalosporanic ring, according to which a 7-ACA amino thiazolyl protected adduct is prepared by acylating said amino group by an aminothiazolyl acetic acid whose amino group has been protected by a phenyl acetyl or a phenoxy acetyl group, the amino group being then deprotected by aqueous hydrolysis in the presence of penicillin G amidase or respectively penicillin V amidase.

Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of .beta.-lactamase enzymes.

Abstract: The invention provides compounds of the formula: ##STR1## wherein the variables are hereinbelow described; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.

Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R, 7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxyme thyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive steps.

Abstract: Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylateThe invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate of the general formula II ##STR1## in which X is the anion of a physiologically acceptable, mono- or polybasic, inorganic or organic acid and the group =N--OH is in the syn-position, pharmaceutical formulations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the use of the cephem derivatives for combating bacterial infections.

Abstract: A compound of the formula: ##STR1## in which R.sup.2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl,R.sup.3 is carboxy or a protected carboxy group,A.sup.5 is lower alkylene which may have a group of the formula: .dbd.N.about.OR.sup.6, wherein R.sup.6 is hydrogen, lower alkenyl, lower alkynyl, lower alkyl or lower alkyl substituted by one or more substituent (s) selected from carboxy, a protected carboxy group, amino, a protected amino group and a heterocyclic group, andX.sup.1 is halogen,or a salt thereof.

Abstract: The invention relates to a process for the preparation of cephem prodrug esters of the formula: ##STR1## in which R.sup.1 is C.sub.1 -C.sub.5 -alkanoyloxy-C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.5 -alkoxycarbonyloxy-C.sub.1 -C.sub.3 -alkyl and X is an inorganic or organic anion, and in which the hydroxyimino group is present in the syn-form.

Abstract: Provided is a process for preparing a cephem compound of the formula: ##STR1## wherein R.sup.3 is hydrogen or methoxy, R.sup.4 is hydrogen or a residue of a nucleophilic compound, R.sup.5 is hydroxyl or a protected hydroxyl, and R.sup.8 is hydrogen or halogen, or a pharmaceutically acceptable salt or ester thereof, which comprises introducing an acyl group of the formula: ##STR2## wherein R.sup.5 and R.sup.8 are as defined above into the amino group of the molecule of the formula: ##STR3## wherein R.sup.3 and R.sup.4 are as defined above or a salt or ester thereof.

Abstract: The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.

Abstract: The invention relates to oxime derivatives of cephalosporanic structure, possessing antibacterial activity.

Abstract: The present invention provides a process for preparing cephem derivatives having the following general formula (I): ##STR1## in which R.sup.1 represents a carboxy group or a protected carboxy group which can form the salt of --COO.sup.- M.sup.+ with an alkali metal ion (M.sup.+) such as sodium, or may represent --COO.sup.- when R.sup.2 has a substituent having positive electric charge such as pyridinium, pyrimidinium or thiazolium,R.sup.2 represents hydrogen, acyloxymethyl, heterocyclic methyl or heterocyclic thiomethyl, each of which can be substituted with appropriate substituents,R.sup.3 represents hydrogen or an amino-protecting group,R.sup.4 represents C.sub.1 -C.sub.4 alkyl or phenyl, or together with the oxygen or phosphorus atom to which it is attached may form a 5- or 6-membered heterocyclic ring, andQ represents N or CH, characterized in that a reactive thiophosphate derivative of thia(dia)zole acetic acid having the following general formula (II): ##STR2## wherein R.sup.3, R.sup.

Abstract: A method for preparing cephalosporm derivatives by reacting cephalosporin alkaline metal salts with organic halide in the presence of quaternary ammonium salts catalyst is disclosed. .DELTA..sup.3 .fwdarw..DELTA..sup.2 isomerization, a side reaction commonly reported in preparation of cephalosporin derivatives was successfully eliminated. The desired .DELTA..sup.3 was obtained as a sole product in the reaction.

Abstract: A method for preparing a new class of protected amino intermediates is provided which utilizes reaction of an imido protected primary amine with a secondary amine. The intermediates thus provided are suitably protected for nucleophilic functionalization on the residue of the primary amine. The desired imido protected amine thus derivatized may be regenerated using acid. Further provided are methods for resolving racemic primary amines. Also provided are .beta.-lactam intermediates protected with the new amino protecting group which are useful in the preparation of .beta.-lactam antibiotics.

Abstract: A compound of formula (I): ##STR1## or a salt thereof, is prepared by reacting 7-aminocephalosporanic acid or a salt thereof, with a solution comprising a compound of formula ROSO.sub.3 H in a compound of formula ROH, and in the presence of at least one compound of formula B(OR).sub.3 or compound of formula CH.sub.2 (OR).sub.2 ; wherein, in each of said compounds of formulae (I), ROSO.sub.3 H, ROH, B(OR).sub.3 and CH.sub.2 (OR).sub.2, R represents an alkyl group having from 1 to 6 carbon atoms.

Abstract: The present application discloses a process for the conversion of penicillin-1-(R)-sulfoxide(s) and/or cephalosporin-1-(R)-sulfoxides in solution, to their corresponding 1-(S)-sulfoxides comprising the step of treating said 1-(R)-sulfoxide with a sufficient amount of an acid anhydride to convert at least some of said 1-(R)-sulfoxide to its corresponding 1-(S)-sulfoxide. Also disclosed is a process for the production of 1-(S)-sulfoxide from penicillin and/or cephalosporin by oxidizing the penicillin or cephalosporin with an oxidizing agent and simultaneously or subsequently adding a sufficient amount of an acid anhydride to convert at least some 1-(R)-sulfoxide to its corresponding 1-(S)-sulfoxide over a time period of from 5 minutes to 2 hours so as to maintain the pH above 3.5 and produce a solution of the corresponding 1-(S)-oxide. In a preferred embodiment, a buffer is incorporated in the solution to provide additional pH control during the reaction.

Abstract: The invention provides complexes of the formula: ##STR1## wherein X is chloro, hydrogen, vinyl, or --CH.sub.3,Z is O;is 0-5;Y is phenyl or 1,4-cyclohexadien-1-yl;R.sub.1 and R.sub.2 are hydrogen or hydroxy, with the proviso that R.sub.1 and R.sub.2 are not both hydrogen andR.sub.3 is --COO.sup.-, --COO(C.sub.1 -C.sub.4 alkyl), --NO.sub.2 or ##STR2## wherein R.sub.4 is C.sub.1 -C.sub.4 alkyl.

Abstract: The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their salts by ester cleavage.The process comprises treating the compound II with formic acid, trifluoroacetic acid, methanesulfonic acid or trifluoromethanesulfonic acid or a mixture of two of these acids in each case.

Abstract: Zinc salts of Cephalosporin C are dissolved in a solution of halides of univalent metals at a temperature of 0.degree.-25.degree. C. and the pH is adjusted to 1-2 prior to being ion exchanged with a sodium form cation-exchange resin packed in a column and being eluted with a water miscible solvent. The column can be further eluted with a solution of halides of univalent metals.

Abstract: A cephalosporin compound substituted in the 7-position with a (cyclo)alkylideneammonio group of formula (II) ##STR1## wherein X' is an anion from an acid HX, R.sub.1 and R.sub.2 are individually a C.sub.1 -C.sub.16 alkyl group, or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a cycloalkylidene ring with up to 8 carbon atoms and a process for the preparation which compounds are useful intermediates.

Abstract: The invention relates to a substantially anhydrous crystalline cefadroxil having a water content between about 0.8% and 3.9%.Such cefadroxil is obtained slurrying a cefadroxil solvate of dimethylacetamide, or of N-methyl-2-pyrrolidone or of monomethylformamide, with isopropyl alcohol with up to 4% of water and preferably in the presence of methanol in an amount lower than 60%, at a temperature of about +45.degree. C. to +55.degree. C. and then filtering the so obtained compound.

Abstract: A process for preparing B-lactam derivatives of the formula (I): ##STR1## wherein R.sup.1 represents hydrogen or a metal salt; and R.sup.2 represents hydrogen, acetoxy methyl, (2,5-dihydro-2-methyl-6-hydroxy-5-oxo-as-triazin-3-yl)thiomethyl or (1-methyl-1-H-tetrazol-5-yl)thiomethyl is disclosed. This process comprises the steps of (a) reacting triphenylphosphine and hexachloroethane or carbon tetrachloride with 2-(2-aminothiazol-4-yl)-2-syn-methoxyimino acetic acid in an organic solvent to give the corresponding acyloxyphosphonium chloride derivative of the formula: ##STR2## (b) acylating a previously silylated derivative of 7-ACA with this acyloxyphosphonium chloride derivative without its isolation.

Abstract: The present invention relates to a process for the preparation of exomethylene cephams, which are useful intermediates in the production of many useful .beta.-lactam antibiotics.More particularly there is provided a process for preparing a compound of formula I ##STR1## wherein n is O or 1, R.sub.1 is hydrogen atom or an organic residue and R.sub.2 is a carboxy protecting group, which process comprises reacting a compound of the formula II ##STR2## wherein X is halogen atom or acetoxy group and R.sub.1 n and R.sub.2 are as defined above with a lanthanide complex.

Abstract: A method for synthesizing .DELTA..sup.3 -7-substituted amino desacetoxy cephalosporanic acid from a penicillin sulfoxide or its alkylsilylated ester derivative is provided. According to the method, penicillin sulfoxide is heated in the presence of an organic ammonium salt catalyst and a copolymer composed of dimethylsilane and urea units until formation of the cephalosporanic acid occurs by ring expansion reaction. The copolymer functions both as a dehydrating agent for removing the water by-product generated from the reaction as well as an esterifying agent for converting penicillin sulfoxide into its dimethylsilyl ester derivative. The method of the invention produces high yields of the cephalosporanic acid and avoids the need for excess dimethylsilyating agents.

Abstract: This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

Abstract: There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R.sub.1 is an organic residue, R.sub.2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group, and n represents 0, 1 or 2.The process comprises reacting a compound of the formula (II): ##STR2## wherein R.sub.2 and n are as defined above, with an inorganic or organic nitrite, in an alcohol R.sub.1 OH, wherein R.sub.1 is as defined above, or in a mixture R.sub.1 OH-organic solvent in the presence of an inorganic or organic acid.The compounds of the formula (I) are known intermediates in the synthesis of human leucocyte elastase inhibitors (HLE).

Abstract: A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with a more desirable protecting group.

Abstract: Provided is a process for 3' acetylation of 3-hydroxymethylcephalosporins under aqueous conditions.

Abstract: Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.

Abstract: The absorption of antibiotics given through oral and rectal routes of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of an ether of a C.sub.6 to C.sub.18 alcohol and a polyoxyethylene glycol together with a second component selected from among polyoxyethylene glycol C.sub.6 to C.sub.18 glyceride esters, C.sub.6 to C.sub.18 carboxylic acids or salts thereof, and esters of two or more C.sub.6 to C.sub.18 carboxylic acids, glycerol and a polyoxyethylene glycol. A carrier and adjuvants are usually included. These compositions can be administered in any convenient oral or rectal dosage form, including tablets, capsules, beadlets and suppositories.

Abstract: The present invention provides a process for protecting an amino group in a compound exposed to nucleophilic reaction conditions in which the imido group used for protection is reacted with a secondary amine to form an acyl group which protects the amino group during exposure to the nucleophilic reaction conditions, after which the acylamino group may be reacted with an acid to reform the imido group so that the compound may then undergo non-nucleophilic manipulations. Also provided is a resolution method in which diasteriometric compounds having the acylamino group as described above are reacted with acid, and as these diasteriomers react at different rates to form the imido group, the reaction may be monitored so as to isolate the desired product at the appropriate point to maximize optical purity.

Abstract: This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.This invention also relates to an intermediate represented by formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3 and n are as defined above.

Abstract: Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity;R.sub.2 is hydrogen, lower alkoxy, lower alkylthio or formamido;R.sub.3 is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;R.sub.4 is an electronegative acidic group; or R.sub.3 and R.sub.4 together form a heterocycle; andR.sub.5 is hydrogen or lower alkyl, except when R.sub.3 and R.sub.4 form a heterocycle, in which case R.sub.5 is hydrogen only; and methods of using same.

Abstract: A process for preparing a well crystallized alkali metal salt of 3, 7-substituted 7-aminocephalosporanic acid derivatives having the general formula: ##STR1## wherein: R1= ##STR2## R.sup.2 =CH3 or C1 M=Na or Kfrom the acid-form derivatives. The process includes preparing a 30% suspension by weight of the acid-form derivative in concentrate alcohol containing 3 to 7% of water by weight, and add an alcoholic solution of alkali base to the suspension under room temperature. The alcohol used to dissolve the base also contains 3 to 7% of water. After a reaction time of 5 to 20 minutes, cool the mixture and let the salt crystallize, and separate the latter from the liquid phase.

Abstract: Cephalexin monohydrate prepared by the silylation of 7-ADCA is obtained in high yield and of improved purity when the silylation step is carried out by refluxing in a solvent having a boiling point of over 100.degree. C.

Abstract: Cephemcarboxylic acid esters of the general formula ##STR1## pharmaceutical preparations which are active against bacterial infections, which contain such cephem derivatives, a process for the preparation of the cephem derivatives and the pharmaceutical preparations, and also the use of the cephem derivatives for combating bacterial infections.

Abstract: Antibacterial compounds of the formula ##STR1## wherein R is a mononuclear carbocyclic aromatic group, a 5-membered aromatic heterocyclic group which contains as the hetero (non-carbon) ring member(s) an oxygen or sulphur atom or an imino or lower alkylimino group and, optionally, one or two nitrogen atoms, or a 6-membered aromatic heterocyclic group which contains one to three nitrogen atoms as the hetero ring member(s); R.sup.1 is hydrogen or a 3-substituent which is usable in cephalosporin chemistry; A is lower alkylene or C.sub.3-7 cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di-(lower alkyl)carbamoyl; Q is lower alkylene or C.sub.3-7 cycloalkylene which is optionally substituted with carboxy, carbamoyl, lower alkylcarbamoyl or di(lower alkyl)carbamoyl, or the group --NR.sup.2 -- or --NR.sup.2 NR.sup.3 --; R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl; p and m are the zero or 1, n is zero, 1 or 2; R.sup.

Abstract: Compounds of general formula (I) ##STR1## (where R.sup.1 is a carboxyl group, a group COO.sup..crclbar. or a blocked carboxyl group;R.sup.2 is an amino or protected amino group; andR is hydrogen or a group of the formula CH.sub.2 X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR.sup.3, where R.sup.3 is hydrogen, a C.sub.1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR.sup.4, where R.sup.4 is a C.sub.1-4 alkyl group optionally substituted by halogen or a C.sub.1-4 alkoxy group; or a pyridinium, 3-carbamoyl-pyridinium or 4-carbamoyl-pyridinium group;B is --S-- or --SO-- (.alpha.- or .beta.-); and the dotted line bridging the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R.

Abstract: Cephalosporin intermediates having a replacable organosulfonylyoxy or heterocyclothio group in the 3-position undergo a carbon alkylation process with organocopper reagents to provide 3-hydrocarbon substituted cephalosporin antibiotics.

Abstract: The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1-dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyltin hydride or actinic radiation at 40.degree. C. to 150.degree. C. to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.

Abstract: Cephalosporin compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are a hydrogen atom or a lower alkyl group of 1-5 carbon atoms and A is a hydrogen atom or a nucleophilic compound residue or pharmacologically acceptable salts thereof have excellent antibacterial activity against Gram positive and Gram negative microorganisms.

Abstract: A method for producing a compound of the formula; ##STR1## wherein R stands for a hydrogen atom, an acyl group or a protective group other than acyl groups, Q stands for a hydrogen atom or an ester residue, Y stands for the residue of a nucleophilic compound and the dotted line shows the double bond at 2- or 3- position of the cephem ring or a salt thereof, characterized by allowing a compound of the formula; ##STR2## [R, Q and the dotted line are of the same meaning as above] or a salt thereof to react with a nucleophilic compound or a salt thereof and a compound of the formula; ##STR3## wherein R.sup.1, R.sup.2, R.sup.3 independently stand for a hydrocarbon group having not more than 8 carbon atoms, or R.sup.1 and R.sup.2, R.sup.1 and R.sup.3 or R.sup.2 and R.sup.

Abstract: The present invention relates to novel cephalosporin compounds having high antimicrobial activity, which are shown by the formula(I), and to a process for preparing them ##STR1## wherein R.sup.1 is a hydrogen atom or an amino protecting group;R.sup.2 is acetoxy; andR.sup.3 is a hydrogen atom or a carboxyl protecting group (wherein when R.sup.2 contains quaternary ammonium, r.sup.2 and R.sup.3 may form a zwitter ion).The present invention also relates to the non-toxic and pharmaceutically acceptable salts of the cephalosporin compounds of the formula (I). Also described are compositions containing the antibiotics according to the present invention.

Abstract: Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.

Abstract: A process is described for producing pure crystalline products, in particular penicillin and cephalosporin, wherein the desired product, prepared according to a known method, is treated with ethanol in one or two steps, whereby the crystallization of the pure product and impurity separation are achieved.

Abstract: A method of producing 3-alkanoyloxymethyl-3-cephem-4-carboxylic acids, which are useful as antibiotics or as intermediates in the synthesis of antibiotics, by reacting a 3-hydroxymethyl-3-cephem-4-carboxylic acid with a saturated fatty acid anhydride in an aqueous medium in the presence of an acid-acceptor base and a 4-(tertiary amino)pyridine.

Abstract: Cephalosporins active as antibacterial agents, and processes for synthesis of such agents, are disclosed.

Abstract: The crystalline ethanol or methanol solvates of cephalexin hydrochloride are isolated in high yield from solutions of cephalexin hydrochloride in substantially anhydrous ethanol or methanol, respectively, by adding miscible C.sub.5 -C.sub.6 alkanes after initiating solvate crystallization. Ethanol or methanol solutions of cephalexin hydrochloride can be prepared by adding gaseous HCl to the respective alcohol slurries of cephalexin monohydrate or the novel crystalline ethanolate or desolvated ethanolate. Alternatively, the cephalexin bis-DMF solvate-derived cephalexin hydrochloride isopropanolate can be used to prepare the crystalline hydrochloride monohydrate in accordance with the disclosed improved method.

Abstract: Process for the production of known 2-oximinoacetamido-3-cephem-4-carboxylic derivatives comprising acylation of 7-amino-3-cephem-4-carboxylic acid derivatives with novel 2-oximinoacetic acid thio esters, as well as such thioesters and their production.

Abstract: Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.

Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing ##STR3## Z representing O, S, or NR.sup.10, and R.sup.2 represents hydrogen or a protective group.