Abstract: The present invention relates to a process for the preparation of crystalline cefuroxime axetil with high purity lecel and optimal diastereomeric ratio. Said process, which comprises the use of a dimethyl carbonate for isolating crystallizing cefuroxime axetil, is particularly suitable for implementing on an industrial scale.

Abstract: There is described the preparation of the new 7&bgr;-[(2-aminothiazol-4-yl)glyoxylamido-3-hydroxymethyl-2-cephem-4-carboxylic acid derivatives, in which the amino group is free or protected by a removable group, and the subsequent conversion of the compounds thus obtained into active cephalosporin precursors either by esterification of the hydroxy group or replacement of the hydroxy group by a halogen atom and, in the latter case, by subsequent replacement of the halogen atom of said 7&bgr;-[(2-aminothiazol-4-yl)glyoxylamido-3-halomethyl-3-cephem-4-carboxylic acid derivatives by the residue of a nucleophilic compound to obtain corresponding, immediate precursors of 7&bgr;-[&agr;-(2-aminothiazol-4-yl-&agr;-methoxyimino]acetamido-3-(substituted)methyl-3-cephem-4-carboxylic acid derivatives.

Abstract: There is provided a process for the preparation of a compound according to Formula (II): which includes the step of cyclising a compound of Formula (III): wherein R1, R2, R3, R4, X and m have meanings which are given in the description.

Abstract: A process for the purification of cefixime via a novel tert-octylamine salt of a cefixime intermediate of formula V which may be crystalline and which may be produced in a one-pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.

Abstract: High purity cefdinir is prepared in a high yield by a process comprising the steps of: treating a cefdinir intermediate with a formic acid-sulfuric acid mixture or a formic acid-methanesulfonic acid mixture to obtain a crystalline salt of cefdinir and reacting the crystalline salt with a base in a solvent.

Abstract: The present invention provides an improved process for the preparation of cefixime of formula (I), with an improved quality having/possessing better color and solubility: the process includes the steps of dissolving the compound of formula (II) in water/water immisible solvent using sodium bicarbonate at a temperature in the range of 0° C. to the 35° C., hydrolyzing with sodium hydroxide at a temperature in the range of 0° C. to 25° C., and acidifying the resultant mass to 2.3 to 3.0 with dilute acid in the presence or absence of solvent at a temperature in the range of 10° C. to 45° C.

Abstract: This invention relates to a novel process for the preparation of 3-cyclic-ether-substituted cephalosporins of formula I 1

Abstract: A compound of formula 1

Abstract: The present invention relates to a process for the preparation of cephalosporin antibiotics of the formula (I) 1

Abstract: The present invention relates to a compound of the formula [I]: 1

Abstract: The invention is concerned with a process for the manufacture of vinylpyrrolidinone-cephalosporin derivatives from 3-amino-pyrrolidine derivatives of the formula 1

Abstract: The present invention relates to an improved process for the preparation of the sterile cefuroxime sodium of formula (I).

Abstract: The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I), also, the invention provides a method for preparation of the thioester derivatives and reaction of the thioester derivatives with cephem carboxylic acids to produce cephalosporin antibiotic compounds having general formula (II).

Abstract: The present invention provides an improved process for the preparation of cefixime of formula (I), with an improved quality having/possessing better color and solubility.

Abstract: A compound of formula wherein W, V, R1, R5, R2, R3 and R4 have various meanings, a process for their production and their use as a pharmaceutical.

Abstract: Highly crystalline, highly filterable sodium Cefoperazone in the form of needle crystal aggregates, obtainable by a process comprising the controlled addition of acetone to a solution of water/acetone/alcohols/sodium Cefoperazone at 20˜40° C.

Abstract: A cephem compound or pharmaceutically acceptable salt thereof represented by the formula I: 1

Abstract: The present invention relates to novel processes for the preparation of 3-methylenecephams. More specifically, the present invention relates to the intramolecular cyclization of penicillin sulfoxide derived monocyclic azetidinone derivatives with organometallic catalysts of the formula III. MEx(H2O)y  (III) wherein: M is Sc, Y, La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Zr, Hf, Th, Nb, Ta, U, Bi, or In; E is O[SO2(C1-C6 polyfluoroalkyl)], N[SO2(C1-C6 polyfluoroalkyl)]2, or C[SO2(C1-C6 polyfluoroalkyl)]3; x is 3; y is 0, 1, 2, 3, 4, 5, 6, 7, 8, or 9.

Abstract: 6(7)-&bgr;-substituted &bgr;-lactam compounds as inhibitors of &bgr;-lactamase activity.

Abstract: Compounds of formula (I): 1

Abstract: The present invention relates to a new method for the preparation of Ceftiofur acid of formula (I), 1

Abstract: The invention is directed towards a process for the preparation of Cefuroxime acid or for a corresponding pharmaceutically acceptable salt or ester. The process comprises the carbamoylation of a Cefuroxime precursor with an activated isocyanate. Additionally, the process is characterized by the fact that a carbonic C1-C4 alkyl ester is used as a solvent for the carbamoylation reaction.

Abstract: A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak—E means the alkali earth metal; and B means the inorganic acid, respectively.

Abstract: A new crystalline form of cefdinir having a dissolution rate less than that of the known crystalline form of the same product.

Abstract: A compound of formula 1

Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug compounds and methods for synthesizing these 1-acyl-alkyl derivatives.

Abstract: The present invention relates to a novel cephalosporin compound, and pharmaceutically acceptable non-toxic salt, physiologically hydrolysable ester, hydrate, solvate or isomer thereof, to a pharmaceutical composition containing the compound and to a process for preparing the compound.

Abstract: Substrates for &bgr;-lactamase of the general formula I 1

Abstract: Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms, as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.

Abstract: A compound of formula 1

Abstract: 1. A process for preparing a 3-alkenylcephem compound or 3-norcephem compound of the formula (3) characterized in that an alkenyl halide of the formula (2), a nickel catalyst, a metal up to −0.3 (V/SCE) in standard oxidation reduction potential and a compound of a metal having a higher standard oxidation reduction potential than the metal are caused to act on a 3-cephem compound of the formula (1) in a solvent wherein R1 is a hydrogen atom or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or carboxylic acid protective group, and X is a halogen atom or the like, R4—Y  (2) wherein R4 is 1-alkenyl having or not having a substituent, and Y is a halogen atom wherein R1, R2 and R3 are as defined above, and R5 is a hydrogen atom or 1-alkenyl having or not having a substituent.

Abstract: A process for preparing cephalosporanic acid derivatives comprises the steps of enzymatically converting a 3-thiolated cephalosporin C compound of formula III: 1

Abstract: The invention provides compounds of formula (I): 1

Abstract: The present invention provides processes for the production of a compound of formula I wherein X, R1 and R2 are substituents conventional in cephalosporin chemistry; especially a compound of formula I is ceftrixone, cefotaxime; e.g., in the form of a salt.

Abstract: An enzymatic process for preparing 3-thiolated 7-aminocephalosporanic acid derivatives comprises the steps of enzymatically converting a 3-thiolated cephalosporin C of the formula I: 1

Abstract: A compound of formula wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent.

Abstract: The invention provides compounds of formula I and IV: 1

Abstract: Disclosed is a process for the preparation of vinyl-pyrrolidinone cephalosporine derivatives of formula Also disclosed are intermediate compounds of formulas wherein R1 and R2 are as defined herein.

Abstract: Provided are fluorescent substrates for &bgr;-lactamases having the general formula I: 1

Abstract: A process for the preparation of Cefuroxime acid (1), which comprises the following steps: (1) Extraction of deacetyl 7-glutaryl ACA (II) aqueous solution at acid pH with organic solvents (for example according to the procedures disclosed in U.S. Pat. No. 5,801,241); (2) drying the resulting solution while preventing lactonization of the intermediate; (3) carbamoylation of the hydroxymethyl group at the 3-position by reaction with chlorosulfonyl isocyanate or similar products; (7) extraction of the carbamoyl derivative from step 3 with water at neutral pH; (8) enzymatic hydrolysis of the amide at the 7-position of the cephalosporanic ring with glutaryl acylase; (6) acylation of the amino group by condensation with 2-furanyl(sin-methoxyimino)acetic acid chloride or mixed anhydride.

Abstract: The process of the present invention and the preparation of the compound of the present invention are illustrated in the following reaction schemes. Except where otherwise indicated, in the reaction schemes and discussion that follow, substituents R1, R2, R3, L, A1, A2 and X are as defined above unless otherwise described.

Abstract: Described are compounds having the formula:

Abstract: 1

Abstract: A compound useful as an anti-bacterial agent, having the formula wherein R2 together with the nitrogen atom to which it is attached forms a cyclic aminoguanidine group or derivative thereof as defined

Abstract: A compound of formula 1

Abstract: The present invention provides compositions comprising improved beta-lactam antibiotics and methods for applying these compositions to inhibit the growth of microbial infections. The improved antibiotics are capable of inhibiting the growth of both antibiotic sensitive and antibiotic resistant microorganisms In addition, the invention provides methods for treating a subject infected with a microorganism by administering the compositions of the invention.

Abstract: This invention relates a process for preparing a compound of formula (I) 1

Abstract: A compound of formula 1

Abstract: A process for preparing 3-alkenylcephem compounds characterized in that 3-alkenylcephem compound of the formula (3) is prepared in a single step by simultaneously conducting reactions of a 3-chloromethylcephem compound of the formula (1) with iodization reagent, alkali metal hydroxide or carbonate, arylphosphine and an aldehyde of the formula (2)  R4—CHO  (2) wherein R1, R2, R3 and R4 are as defined in the specification.

Abstract: A process in the isolation of 7-aminocephalosporanic acid (7-ACA) from an alkaline, neutral or slightly acidic medium in the presence of an additive, e.g. selected from the group comprising organic carboxylic acid esters, polymeric glycols, polyacryls, amines and polyamines, melamin-formaldehyde resins or amino acids and esters thereof to obtain 7-ACA agglomerates and or rosettes.