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4622394 |
Oxygen analogs of cephalosporins
In accordance with this invention, it has been found that the oxygen analog of 7-amino-cephalosporanic acid and biologically active derivatives thereof can be formed from esters of...
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4606865 |
Methods for the preparation of α-bromodiethylcarbonate
The novel compound α-bromodiethylcarbonate, novel methods for the preparation thereof, its use in the preparation of 1-ethoxycarbonyloxyethyl esters of penicillins and cephalosporins, and...
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4604457 |
2-substituted cephem derivatives and process for preparing the same
A 2-substituted cephem derivative represented by the formula ##STR1## wherein R 1 represents a substituted or unsubstituted phenyl group, substituted or unsubstituted phenylmethyl group or...
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4584371 |
Catalytic process for preparing 3-ester-methyl cephalosporins from desacetyl-7-aminocephalosporanic acid
3-(Activated ester)methyl-3-cephem-4-carboxylic acids are prepared by the direct reaction of a 3-hydroxymethyl-3-cephem-4-carboxylic acid with an activated-O-ester-methyl forming acylating agent in...
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4574152 |
Cephalosporin compounds
Ternary complexes comprising a 7-[D-5-amino-5-carboxypentanamido] cephalosporin complexed with copper (II) ions and an organic nitrogen base as well as a process for their preparation are...
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4558123 |
3-Exomethylene cephalosporins
3-Acetoxymethylcephalosporins are converted to 3-exomethylene cephalosporins by reaction with a metal and a bound proton source.
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4537886 |
β-lactam antibacterial agents and compositions containing them
A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R 1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring...
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4504657 |
Cephadroxil monohydrate
A novel crystalline monohydrate of 7-[D-α-amino-α-(p-hydroxyphenyl)acetamido]-3-methyl-3-ceph
em-4 -carboxylic acid is prepared and found to be a stable useful form of the cephalosporin...
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4502988 |
Oxidation process
Penicillin and cephalosporin sulfides and sulfoxides are readily converted to sulfones in the presence of ruthenium tetroxide.
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4496561 |
Cephalosporin derivative
A cephalosporin derivative having an antibacterial activity similar to a cephalosporin antibiotic in living bodies without affecting the intestinal bacterial colonies, a method for preparing the...
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4490370 |
Naphthylglycyl cephalosporin derivatives
Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and are particularly useful as oral treatments for upper respiratory infections.
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4489072 |
Cephalosporins
Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl...
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4486425 |
7-[2-(2-A minothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]-3-methoxymethyl-3-cephem -4-carboxylates
Compounds of formula (I): ##STR1## wherein: R 1 represents a lower alkyl group selected from methyl groups and ethyl groups; R 2 represents a hydrogen atom or a methyl group; and R 3 ...
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4482435 |
Process for preparing thiazolidine compounds
This invention provides a process for preparing a thiazolidine compound of the formula ##STR1## wherein R 1 represents a hydrogen atom, alkyl group, aralkyl group, aryl group or aryloxymethyl...
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RE31730 |
Process for the preparation of the crystalline monohydrate of 7-(D-α-aα-(p-hydroxyphenyl)acetamido)-3-methyl-3-cephem-4-ca rboxylic acid
A novel crystalline monohydrate of 7-[D-α-amino-α-(p-hydroxyphenyl)acetamido]-3-methyl-3-caph
em-4 -carboxylic acid is prepared and found to be astable useful form of the cephalosporin antibiotic...
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4482710 |
Process for preparing 3-alkoxymethylcephalosporin derivatives
The acetoxymethyl group at the 3-position of 3-acetoxymethylcephalosporanic acids and salts thereof may be replaced by an alkoxymethyl group, by reacting the 3-acetoxymethylcephalosporanic acid or...
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4477660 |
7-(S)-Acylaminocephalosporin sulfones and process
This invention encompasses 7-(S)-acylamino-3-acetoxymethyl-3-cephem-4-carboxylic acid sulfones and the epimerization process for making them. The epimerization process employs an organic nitrogen...
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4474780 |
Crystalline cephalosporin
7-(D-2-Naphthylglycylamido)-3-methyl-3-cephem-4-carboxylic acid tetrahydrate is a stable crystal form of a potent orally active gram positive antibiotic.
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4471115 |
Water soluble derivatives of cephalex and process for their preparation
The water soluble derivatives of cephalexin, having general formula: ##STR1## wherein X represents an alkali metal or the organic nitrogen containing cation of a basic aminoacid, combine the...
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4468514 |
Preparation of 3-bromocephalosporins from thiazoline azetidinones
Thiazoline azetidinones are converted in good yield to 3-bromo-3-methylcephams by treatment with a bromine source and dimethyl sulfoxide.
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4468394 |
Cephalosporin compounds
A compound represented by the formula: ##STR1## wherein R 1 is hydrogen or methoxy; R 2 is hydrogen or hydroxy; R is ##STR2## wherein R 3 and R 4 are hydroxy or acyloxy, Y is oxygen, sulfur or...
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4465631 |
5-Substituted-3-isoxazolecarboxylic acid derivatives
A 5-substituted-3-isoxazolecarboxylic acid derivative of the general formula: ##STR1## wherein X stands for a phenyl group, thienyl group, furyl group or pyridyl group, each of which optionally may...
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4465831 |
Ketoiminocephalosporin derivatives
There is described a new class of ketohydroxyimino derivatives of cephalosporins of the formula ##STR1## wherein: R is an alkyl radical having from 2 to 4 carbon atoms, a phenyl, or a 5-membered...
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4463172 |
Process for producing 2-methyl cephem-2-em and 2-methylcephem-3-em derivitaves
Novel 2-methylcephalosporin derivatives and production thereof. These cephalosporin derivatives exhibit excellent antibacterial activities against gram-positive and gram-negative bacteria, thus...
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4462999 |
7-Acylamino-3-substituted cephalosporanic acid derivatives and processes for the preparation thereof
Anti-microbial cephalosporins of the formula ##STR1## in which R 2 is methoxymethyl or methylthiomethyl, and R 6 is carboxy (lower) alkyl have been prepared.
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4459405 |
Desacetylcephalosporin sulfones
7-(S)-Acylamino-3-hydroxymethyl-3-cephem sulfones are disclosed. These compounds are intermediates in the synthesis of 1-oxa β-lactam antibiotics.
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4456755 |
7-Oxygen analogs of cephalosporins
In accordance with this invention, it has been found that the oxygen analog of 7-aminocephalosporanic acid and biologically active derivatives thereof can be formed from esters of...
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4455306 |
Method for concentrating β-lactam antibiotic solution
The present invention relates to a method for concentrating a dilute aqueous solution of a β-lactam antibiotic which is readily susceptible to heat, by subjecting a dilute aqueous solution of a...
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4447602 |
Process to prepare 7-substituted cephalosporins or 6-substituted penicillins
A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated...
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4446318 |
Method for producing 7-aminocephem compounds
An improvement, in per se known method for producing 7-aminocephem compound being important intermediate for producing antimicrobial substances, represented by the formula: ##STR1## wherein R 1 is...
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4436596 |
N-Substituted-2-(R)-(sulfinic acid)-3-(S)-(acylamido)-4-oxo-azetidines and process
N-substituted-2-(R)-(sulfinic acid)-3-(S)-(acylamino)-4-oxo-azetidines, which are useful as intermediates in 1-oxa β-lactam antibiotics, are synthesized by electrolytic reduction of...
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4426520 |
3-Carbamoyloxy-cepham-4-carboxylic acid derivatives
Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the...
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4400509 |
Silylation process
An improved process for the trimethylsilylation of organic compounds with at least one active hydrogen atom with hexamethyldisilazane, the improvement comprising effecting the reaction in the...
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4391974 |
Water soluble cephadroxyl salt
A new water soluble cephadroxyl salt and the process for the preparation thereof are disclosed.
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4388460 |
Cephalosporine desacetoxy esters and salts thereof
Cephalosporine desacetoxy esters having the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R 1 is selected from the group consisting of ##STR3## Such esters and...
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4385178 |
Process for producing 7-(substituted)amino-3-substituted thiomethyl cephem carboxylic acids
This disclosure relates to a novel process for producing 7-(substituted)amino-3-substituted thiomethyl cephem carboxylic acids which are intermediate products of cephalosporins being valuable...
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4385177 |
Cephalosporins having a carbamoylalkoxyiminoarylacetamido group at 7-position
Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R a and R b , which may be the same or different, are each selected from hydrogen, C 1 -4...
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4380630 |
N-Carboxy cefadroxil sodium salt
N-carboxy cefadroxil disodium salt having formula ##STR1## Said salt is endowed with antibiotic activity and can be administered parenterally.
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4369312 |
Method of producing oxo-containing azetidinone compounds
This invention relates to a novel method of producing oxo-containing azetidinone compounds, or salts thereof, or hydrates thereof, said compounds having utility as antimicrobial agents and as...
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4366315 |
Process for preparing 3'bromo-desacetoxycephalosporanic acid sulfoxide compounds
An improved process for the preparation of 3'-bromo-desacetoxycephalosphoranic acid sulfoxide compounds comprising protecting the 4-carboxy group of a 3'-unsubstituted cephalosporanic acid...
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4363807 |
Cepham compounds
This invention relates to novel cepham compounds of antimicrobial activity, useful as intermediates in the preparation of antibiotics, said novel cepham compounds being of the formula: ##STR1##...
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4358588 |
Process for preparing cephalosporanic acid compounds
A process for the preparation of [D-α-amino-p-hydroxyphenylacetamido]-penicillanic acid or cephalosporanic acid compounds comprising reacting a compound having a formula selected from the group...
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4354023 |
Cefadroxil acetylcysteinate salt
Salts of cefadroxil with an amino acid selected from the group consisting of L-lysine, L-arginine and acetylcysteine. Said salts are obtained by reacting an aqueous suspension of cefadroxil with an...
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4354022 |
Process for preparing 3-methylenecepham compounds or a salt thereof
A new process for preparing 3-methylenecepham compounds of the formula: ##STR1## wherein R 1 is amino or a protected amino group, and R 2 is a carboxy or a protected carboxy group, or a salt...
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4350692 |
3,7-Disubstituted-3-cephem-4-carboxylic acids
Preparation of pharmaceutical composition comprising, treatment of human and animal diseases with, and compounds of, 3,7-disubstituted-3-cephem-4-carboxylic acid.
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4347358 |
Cephalosporin intermediates
Novel bromo-substituted deacetoxycephalosporins of the formula ##STR1## wherein R 1 is selected from the group consisting of benzamido, formamido, phenylacetamido and phenoxyacetamido, R 2 is...
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4346219 |
Process for preparing desacetoxycephalosporanic acid
Process for preparing 7-ADCA and 7-(N,N-disubstituted)aminodesacetoxycephalosporins which comprises reacting 7-ACA or an N,N-disubstituted derivative thereof with a tri-(C 1 -C 6 alkyl)silane in...
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4338439 |
7-[2-[(Substituted benzoyl]amino]acetamido]cephalosporins
Cephalosporin antibiotics of the formula ##STR1## wherein R is cyclohexadienyl, phenyl or substituted phenyl, 2-thienyl, 3-thienyl, 2-furyl or 3-furyl; R 1 is a substituted phenyl having 1 to 4...
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4336376 |
Process for the preparation of 7-(D(-)-alpha-amino-p-hydroxyphenylacetamido)desacetoxycephalosporanic acid
There is described a process for the preparation of 7-(D(-)-alpha-amino-p-hydroxyphenylacetamido)desacetoxycepha
losporanic acid in which a...
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4334064 |
Cephalosporin vinyl halides
7-Acylamido-2-halomethylidene-3-methyl and 3-acetoxymethyl-3-cephem-4-carboxylic acids and esters are prepared via reaction of the corresponding 2-exomethylene-3-cephem ester sulfoxides with chloro...
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