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7615631 |
Crystalline solvate of cefuroxime acid
Crystalline acetonitrile solvate of cefuroxime acid, useful for preparing the antibiotic cefuroxime sodium salt.
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7592447 |
Process for production of intermediates for use in cefalosporin synthesis
A process for the production of intermediates having a formula IA
that can be used for the synthesis of cephalosporins, such as cefepime of formula V. The intermediates of formula IA are...
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7531650 |
Cephalosporin salts in crystalline form
The present invention relates to cephalosporin of formula (I) in crystalline form. The compound of formula (I) in crystalline form is useful as antibiotics having potent and broad antibacterial...
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7507813 |
Amorphous cefuroxime axetil and preparation process therefore
A novel process for the preparation of amorphous cefuroxime axetil particles and the amorphous cefuroxime axetil particles therefrom are disclosed in the invention. Specifically, the invention is...
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7488724 |
7-alkylidene-3-substituted-3-cephem-4-carboxylates as beta-lactamase inhibitors
The invention provides compounds of formula (I):
wherein: R 1 -R 4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for...
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7479556 |
Process for producing Cefepime and cephalosporin analogues
Process for producing Cefepime, Cefpirome and Cefquinome, whereby a cephalosporin containing a quaternary ammonium group is reacted with thiourea to provide the aforesaid cephalosporins.
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7452990 |
Intermediates for synthesis of cephalosporins and process for preparation of such intermediates
A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics
wherein
X is chlorine or...
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7427680 |
Fluorogenic substrates for BETA-lactamase gene expression
Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing...
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7405294 |
Intermediate cefdinir salts
Disclosed are salts of the general formula (I)
wherein R 1 , R 2 and B are defined in the description. These salts are useful intermediates for the preparation of cefdinir. Also, disclosed are...
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7396926 |
Beta-lactamase substrates having phenolic ethers
Provided are fluorescent substrates for β-lactamases having the general formula I:
in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R′ is selected from the group consisting of...
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7384928 |
Broad spectrum cephem compounds
A compound of the formula:
(wherein,
T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower...
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7355040 |
Process for the preparation of cephalosporin compounds and synthetic intermediates
There is provided a process for the preparation of a compound according to Formula (II):
which includes the step of cyclizing a compound of Formula (III):
wherein R 1 , R 2 , R 3 , R 4 , X...
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7339055 |
Process for the preparation of cephalosporin antibiotic
A process for the preparation of cephalosporin antibiotic of the formula (I)
which comprises:
(i) activating the compound of formula (III) as acid halide in an organic solvent
(ii)...
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7250508 |
Cefdinir intermediate
7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetami
do]-3-vinyl-cephem-4-carboxylic acid of formula I
in the form of a crystalline salt and use thereof, e.g. in the preparation of pure...
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7244842 |
Amorphous hydrate of a cephalosporin antibiotic
A process for the preparation of cefdinir of the formula (I) the said process comprising the steps of: i) condensing 7-amino-3-cephem-4-carboxylic acid of the formula (XII) wherein R1 is as defined...
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7192943 |
Cephem compounds
The present invention relates to a compound of the formula [I]:
wherein R 1 is lower alkyl or hydroxy(lower)alkyl, and R 2 is hydrogen or amino protecting group, or R 1 and R 2 are bonded...
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7179801 |
Cephem compounds
The present invention relates to a compound of the formula [I]: wherein A is lower alkylene or lower alkenylene; R 1 is lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl,...
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7173126 |
Crystalline cefdinir salts
Cefdinir crystalline salts of formula (I),
in which n ranges from 1 to 3, the preparation and use thereof for the preparation and purification of cefdinir are herein disclosed. The salts of...
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7157576 |
Crystalline acid salts of cefdinir and process for preparing cefdinir using same
High purity cefdinir is prepared in a high yield by a process comprising the steps of: treating a crystalline salt of a cefdinir intermediate with a formic acid-sulfuric acid mixture or a formic...
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7157575 |
Substrates for β-lactamase and uses thereof
Substrates for β-lactamase of the general formula I
in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R′ is selected from the...
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7129232 |
Cephem compounds
The present invention relates to a compound of the formula [I]:
wherein
R 1 is lower alkyl, hydroxy(lower)alkyl or halo(lower)alkyl, and R 2 is hydrogen or amino protecting group, or R...
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7112672 |
Process for the selective preparation of 3-(z) propenyl-cephem compound
A 3-(Z)-propenyl cephem compound is selectively prepared by reacting a phosphoranylidene cephem compound with acetaldehyde in the presence of a base in a solvent mixture comprising diethyl ether,...
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7105659 |
Process for preparing cefdinir
The present invention relates to a novel process for the preparation of a cefdinir
by reacting O-acetyl thioester of Formula I
with
in the presence of a base in suitable solvent wherein...
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7071329 |
Process for preparing cephalosporins with salified intermediate
Cephalosporins may be conveniently prepared by a process in which a benzathinium salt of formula (V)
wherein:
Z is benzathine; and X and R 2 are as defined in the specification, is...
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7064199 |
Process for the manufacture of 3-amino-pyrrolidine derivatives
The invention is concerned with a process for the manufacture of vinylpyrrolidinone-cephalosporin derivatives from 3-amino-pyrrolidine derivatives of the formula
wherein
R 1 signifies...
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7064198 |
Method for preparation of cefuroxime axetil
A process for preparation of cefuroxime axetil of formula (I) of at least 96% purity and substantially free of analogous Δ 2 -isomer of formula (II) and other impurities. The process comprises
...
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6919449 |
Process for the preparation of cephalosporin intermediate and its use for the manufacture of cephalosporin compounds
The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III)
by...
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6916801 |
7-Alkylidene-3-substituted-3-cephem-4-carboxylates as β-lactamase inhibitors
The invention provides compounds of formula (I):
wherein: R 1 -R 4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for...
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6906187 |
Manufacture of cefalosporins and intermediates
There is described a process for the preparation of 3-disubstituted cepham-4-carboxylic acid derivatives of formula I
wherein R″ is 4-methoxybenzyl, X is the residue of a thioether and Z is...
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6897304 |
Cephem compounds and ESBL-detecting reagents containing the same
A cephem compound or pharmaceutically acceptable salt thereof represented by the formula I:
wherein R 1 and R 2 may be the same or different and each represent hydrogen atom, nitro or cyano;...
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6894162 |
Intermediates in cephalosporin production
Cefuroxime in the form of a salt with n-butylamine; and its use for the production of cefuroxime axetil or for the production of the sodium salt of cefuroxime.
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6878827 |
Process for producing anhydride of aminothiazole derivative
This invention provides a novel industrial process for preparation of an anhydride of 2-(2-aminothiazole-4-yl)-2-hydroxy compound.
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6835829 |
Purification process
Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.
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6833452 |
Process for the preparation of highly pure crystalline (R,S)—cefuroxime axetil
A process for the preparation of highly pure crystalline form of cefuroxime-1-acetoxyethyl ester (cefuroxime axetil) from cefuroxime by reacting an amine salt of cefuroxime with an esterifying...
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6825345 |
Process for purification of a cephalosporin derivative
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...
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6800755 |
Process for the preparation of cefixime
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...
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6693095 |
Antibacterial substituted 7-acylamino-3-(methylhydrazono) methyl-cephalosporins and intermediates
A compound of formula wherein W, V, R 1 , R 5 , R 2 , R 3 and R 4 have various meanings, a process for their production and their use as a pharmaceutical.
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6683176 |
Intermediates for and synthesis of 3-methylene cephams
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...
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6642378 |
Process for the synthesis of beta-lactam derivatives
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...
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6642377 |
Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates
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...
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6583133 |
Propenyl cephalosporin derivatives and process for the manufacture thereof
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...
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6576761 |
Process for the preparation of cephem compounds
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...
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6552186 |
β-lactam production
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...
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6504025 |
Process for the preparation of vinyl-pyrrolidinone cephalosporin derivatives
Disclosed is a process for the preparation of vinyl-pyrrolidinone cephalosporine derivatives of formula Also disclosed are intermediate compounds of formulas wherein R 1 and R 2 are as...
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6440957 |
Cephalosporines having cyclic aminoguanidine substituents as antibiotics
A compound useful as an anti-bacterial agent, having the formula wherein R 2 together with the nitrogen atom to which it is attached forms a cyclic aminoguanidine group or derivative thereof as...
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6417351 |
Process for producing 3-alkenylcephem compounds
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...
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6414140 |
Process for the production of 3-vinyl cephalosporins
A process for the production of a 3-vinylcephalosporin compound of formula I wherein R 1 and R 2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula...
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6407091 |
β-lactamase inhibiting compounds
The invention provides compounds of formula I and IV: wherein R 1 -R 11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for...
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6399770 |
Preparation of β-hydroxy esters using ammonium borohydrides
A process for preparing a β-hydroxyester comprising reducing a β-keto ester in the presence of a salt of ammonium borohydride.
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6384214 |
Process for producing cephalosporin derivatives
The present invention is concerned with a novel process for the manufacture of cephalosporin derivatives of the formula by converting a phosphonium salt into the corresponding ylide and reacting...
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