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5254680 |
Process for the preparation of 7 alpha-alkoxycephem derivatives
There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R 1 is an organic residue, R 2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group,...
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5221739 |
Acetylation of 3-hydroxymethyl cephalosporins
Provided is a process for 3' acetylation of 3-hydroxymethylcephalosporins under aqueous conditions.
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5162524 |
Processes for making cephems from allenylazetidinone derivatives
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...
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5162522 |
Method for producing cephem compounds
A method for producing 3-(3-oxobutyryloxymethyl)-3-cepham-4-carboxylic acids which are antibiotics or intermediates for the synthesis of antibiotics, at a low temperature in a very short period of...
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5159070 |
Process for the preparation of derivative of 7-[(2-hydroxyimino)-acetamido]-cephalosporanic acid
A novel process for the preparation of syn isomers of cephalosporanic acid derivatives of the formula ##STR1## comprising reacting first in a solvent and optionally in the presence of a base, a...
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5159071 |
Process for the manufacture of 7-amino-3-exomethylene-3-cepham-4-carboxylic acid ester
A one-pot process for preparing 7-amino-3-exomethylene-3-cepham-4-carboxylic acid ester (II) comprises: (a) reacting 7-acylamino-3-exomethylene-3-cepham-1-oxide-4-carboxylic acid ester (I) with a...
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5142040 |
Process for preparing a 3-formylcephem derivative
The present invention provides a process for preparing a 3-formylcephem derivative represented by the formula (2) ##STR1## which comprises oxidizing in the presence of oxygen a 3-halomethylcephem...
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5142043 |
Process for preparing cephalexin monohydrate
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...
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5142042 |
Process for preparing well crystallized alkali metal salts of 3, 7-substituted 7-aminocephalosporanic acid derivatives
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 2 =CH3 or C1...
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5132419 |
Process for the preparation of 7-amino-3-((Z)-1-propen-1yl)-3-cephem-4-carboxylic acid
(7-APCA) having the formula (I) ##STR1## which is an important synthesis intermediate in the preparation of cephalosporin-like antibiotics, is prepared by treating a compound of the formula (II)...
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5126446 |
Process for 3-exomethylenecepham sulfoxide esters
3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-amino-1-azetidinyl)-3-b
utenoic acid esters under anhydrous conditions...
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RE33948 |
β-lactam antibiotics
Antibacterially active and animal growth-promoting novel β-lactam compounds of the formula ##STR1## in which R 1 represents the radical ##STR2## Y representing N or CR 9 , or Y--R 7 representing...
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5112967 |
Process for synthesizing antibacterial cephalosporin compounds
A process for synthesizing 3-acryloxymethyl antibacterialcephalosporin compounds of formula ##STR1## wherein R is hydrogen or a carboxylic acid protecting group; R 1 is hydrogen or an acyl group;...
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5109132 |
Process for the preparation of 3-exomethylene cepham derivatives
A process is provided for the preparation of 3-methylene and 3-halomethylene cepham derivatives via 3-phosphoniomethyl-3-cephem derivatives, which in turn can be prepared from 3-halomethyl-3-cephem...
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5095107 |
Process for cleavage of esters during the production of cephalosporins
Superior method for the removal of the methyl or ethyl ester group from cephalosporin and carbacephalosporin carboxylic acids.
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5077286 |
Beta-lactam derivatives of the 4-acylcephem sulphone and 3-acylpenam sulphone-type
Compounds of formulae Ia and Ib ##STR1## wherein A is hydrogen atom or an organic residue, R 1 is halogen atom, or an organic group, R 2 is hydrogen or halogen atom, C 1 -C 4 alkyl or alkoxy...
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5043439 |
Process for production of cephalosporins
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...
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5037975 |
Cephalosporin free radical compounds
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...
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5036064 |
Cephalosporins with sulfur-containing oxyimino side chain
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...
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5034522 |
Method for the production of 3-methyl cephem derivatives
A method for obtaining improved cophalexin monohydrate or cephradine monohydrate yields and purities in the syntheses of such materials by the acylation of silyl esters of 7-ADCA, which involves...
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5034521 |
Process for preparing 3-substituted methyl-3-cephem-4-carboxylic acid
A novel process is disclosed for preparing a 3-substituted methyl-3-cephem-4-carboxylic acid or pharmaceutically acceptable salt thereof. The process comprises reacting a...
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5023331 |
Cefadroxil solvates
The invention relates to a novel crystalline cefadroxyl hemihydrate having a K.F. between about 3.5 and 2.0%: such compound is more stable than other cefadroxyl molecules. The novel cefadroxyl is...
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5003064 |
Method for the preparation of monohydrate
Cefadroxil monohydrate is prepared by solubilizing 7-[D-(-)-α-benzyloxycarbonylamino-α-(p-hydroxyphenyl)aceta
mido ]-3-methyl-3-cephem-4-carboxylic acid by silylation or by salification in an...
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4994454 |
Cepham derivatives
A process is provided for the preparation of 3-methylene and 3-halomethylene cepham derivatives via 3-phosphoniomethyl-3-cephem derivatives, which in turn can be prepared from 3-halomethyl-3-cephem...
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4992541 |
Process for the preparation of 1,1-dioxo-7-substituted cephems
The present invention relates to an improved process for the preparation of the compounds of formula (I) ##STR1## which involve the direct oxidation without N-protection of the compound of the...
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4983732 |
Method of deprotection of 3-amino azetidinones
A method for preparing 2-amino-β-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-β-lactam is further acylated with a...
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4980464 |
Method for production of cephalosporin compounds
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...
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4971961 |
Cephalosporin compounds and antibacterial agents
This invention provides cephalosporin compounds represented by the following general formula: ##STR1## wherein R 1 and R 2 are same or different hydrogen atom or a lower alkyl group of 1 to 5...
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4962195 |
Solvate of cefadroxyl
The invention relates to a novel crystalline cefadroxyl hemihydrate having a K.F. between about 3.5 and 2.0%: such compound is more stable than other cefadroxyl molecules. The novel cefadroxyl is...
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4950753 |
Process for 3-exomethylenecepham sulfoxide esters
3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-acylamino-1-azetidinyl)
-3-butenoic acid esters under anhydrous...
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4945159 |
Formation of lactams and other amides under mild conditions by action of cyanogen
A method for the formation of intramolecular amide bonds by the action of cyanogen, under mild reaction conditions, in the preparation of cyclic amides, including lactams, in biologically active...
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4931555 |
Disulfide substituted oxazetidine derivatives
A process for producing a 2-cephem or 3-cephem derivative compound of the formula: ##STR1## wherein R 1 represents a substituted or unsubstituted amino radical and R 4 represents hydrogen or a...
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4921954 |
Process for the preparation of cephem compounds
Process for the preparation of 7β-amino-3-substituted methyl-3-cephem-4-carboxylic acid derivatives, new intermediates comprising 7β-(cyclo)alkylideneammonio-3-halomethyl-3-cephem-4-carbox ylic...
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4912211 |
Method for producing pure crystalline antibiotic products
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...
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4904776 |
Method for producing crystalline cefadroxil hemihydrate
The invention relates to a method for producing crystalline cefadroxil hemihydrate. According to the method a cefadroxil solvate is slurried with a mixture methanol:isopropyl alcohol 30:70 to 70:30...
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4902793 |
Process for preparing 3-alkoxymethylcephalosporins
A process for preparing 3-alkoxymethylcephalosporins which are useful as an intermediate for various cephalosporin derivatives having a high antimicrobial activity is disclosed. According to the...
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4898938 |
Method for preparing crystalline cefadroxil monohydrate
The invention relates to a method for preparing crystalline cefadroxil monohydrate. According to such a method a cefadroxil solvate is slurried with isopropyl alcohol containing less 6% to 18% of...
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4866169 |
3-substituted-8-oxo-7-substituted-thioxomethylamino-5 -thia-1-azabicyclo-(4.2.0)oct-2-ene-2-carboxylic acid, diphenylmethyl esters
Diphenylmethyl esters of cephalosporins, and processes for synthesizing such, are described and disclosed.
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4853468 |
Process for the preparation of cephem derivatives
This invention provides azetidinone derivatives represented by the formula ##STR1## and processes for preparing the same. The azetidinone derivatives are used as the intermediates for producing...
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4847373 |
Production of 3-allyl- and 3-butenyl-3-cephems
There is disclosed a process for the production of certain 2-allyl- and 3-butenyl-3-cephem derivatives by coupling a 3-chloromethyl-3-cephem with a hydrocarbyltributystannane in the presence of...
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4835267 |
Process for the preparation of cephalosporin derivatives
The present invention relates to an improved process for producing cephalosporin derivatives of formula (I), the 3-position of which being substituted by acetoxymethyl or tetrazolylthiomethyl and...
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4775751 |
Process for cephalexin hydrochloride alcoholates
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,...
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4717768 |
Process for separation of syn and anti oxime isomers of cephalosporin-compounds
A process for the separation of a mixture of syn and anti oxime isomers one from the other which comprises adsorbing said mixed oxime isomers onto a non-functional macroreticular adsorption resin,...
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4716227 |
Process for manufacturing cephalosporin esters
Cephalosporin esters of the formula ##STR1## wherein R 2 is hydrogen or acyl and R 1 is a group which is readily removable by hydrolysis, and pharmaceutically acceptable acid addition salts of...
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4695627 |
Cephalosporin deoxygenation process
A process for the preparation of 7β-acylamino-3-substituted-3-cephem-4-carboxylic acid compounds comprising reacting at -70° C. to 0° C. in an inert organic solvent phosphorus pentachloride with...
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4667027 |
Cephem compounds and their production
A compound of the formula: ##STR1## wherein R 1 stands for hydrogen or formylamino, R 2 is a residue of amino acid selected from the group consisting of serine and alanine, or a peptide of at...
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4661590 |
Substituted vinyl cephalosporins
3-[(Z)-1-Propen-1-yl]-7-acylamido cephalosporins in which the 7-acyl group is phenylglycyl or substituted phenylglycyl are orally active antibiotics against Gram+ and Gram- bacteria.
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4656264 |
Bicyclic azetidinone intermediates
An azetidinone compound represented by the formula ##STR1## wherein R 1 represents a substituted or unsubstituted phenyl group, R 2 represents a carboxyl-protecting group, X represents a hydrogen...
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4640798 |
Intermediates for the preparation of penicillin and cephalosporin compounds
There is described a process for preparing a sulphoxide of the formula ##STR1## in which R 1 , R 2 , R 3 and R 4 , taken individually, are alkyl, alkoxy or aryl groups, X is an alkylene group, R 5...
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4625021 |
High yield process for preparing beta-lactam antibiotics having a high purity degree
A high yield process for preparing beta-lactam antibiotics having a high purity degree, in particular derivatives of the cephalosporanic and penicillanic acids, of the formula: ##STR1## by...
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