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4334065 Cephalosporin intermediates  
7α-(Dimethylamidino)-3-cephem ester 1α-oxides represented by the formula ##STR1## wherein R is hydrogen or acetoxy and R 1 is a carboxy protecting group, are prepared via DBU epimerization of...
4326071 Halomethyl derivatives of gamma-aminobutyric acid and related compounds  
Novel compounds of the following general formula are useful pharmacological agents: ##STR1## wherein Y is FCH 2 - or F 2 CH-; R 1 is hydroxy, a straight or branched alkoxy group of from 1 to 8...
4323704 αAcetylene and α-vinyl derivatives of amino acids  
Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R 1 is --C.tbd.CH or --CHCH 2 ; R 2 is hydrogen or COR wherein R is hydroxy, a straight or branched...
4323676 Process for preparing cephalosporins  
Novel 3-acyloxymethyl-cephem compounds of the formula: ##STR1## wherein R 1 is hydrogen or an acyl group; W is acetonyl, or a group represented by --X--COOH or --X--OH (X is an organic residue) or...
4322526 Process for producing 7-aminocephalosporanic acid  
Novel Cephalosporin C derivatives, their production and their use in isolating Cephalosporin C from culture filtrates for subsequent conversion of 7-aminocephalosporanic acid.
4322347 2-Carbamoyloxymethyl-penicillin derivatives  
Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the...
4320055 Process for penicillin epimerization  
6β-acylaminopenicillin-1β-sulfoxides are epimerized to 6α-acylaminopenicillin-1β-sulfoxides using triethylamine and chlorotrimethylsilane. The 6α-acylaminopenicillin-1β-sulfoxides produced in...
4312982 α-Acylureidocephalosporins and salts and esters thereof  
Compounds which are clinically important cephalosporins and salts and esters thereof having a wide spectrum of activity against Gram-positive bacteria but especially against Gram-negative bacteria...
4310459 Process for producing carbamoyl substituted penams and carbamoyl substituted cephams from penicillin sulfoxide esters  
Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the...
4308381 Cephem compounds  
Novel 3-acyloxymethyl-cephem compounds of the formula: ##STR1## wherein R 1 is hydrogen or an acyl group; W is acetonyl, or a group represented by --X--COOH or --X--OH (X is an organic residue) or...
4304717 Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives  
This invention relates to a process for the preparation of acid amides having the formula (I) or their salts ##STR1## wherein R 1 is hydrogen or an easily removable ester-forming or salt-forming...
4299955 Process for preparing derivatives of 7-amino-desacetoxy cephalosporanic acid  
Process for preparing cephalexine monohydrate and cephadroxyl monohydrate, according to which a reaction is carried out of a mixed anhydride prepared from a Dane salt of phenylglycine or...
4298529 Alkoxyimino dioxy butyric acid derivatives  
The invention relates to new antimicrobially active 3-cephem compounds, processes for preparing such compounds, new intermediate compounds comprising alkoxyimino dioxy butyric acid derivatives...
4296112 Cephalosporins  
A cephalosporanic acid of the general formula ##STR1## wherein A represents ##STR2## and the pharmaceutically acceptable salt and ester thereof.
4286088 Process for preparing 7-aminocephalosporins  
7-Aminocephalosporin of the formula: ##STR1## wherein R 2 is 3-oxobutyryloxy group, 1-methyl-1H-tetrazol-5-ylthio group or 1-(2-dimethylaminoethyl)-1H-tetrazol-5-ylthio group, or its salt is...
4283531 Synthesis of β-lactams having a substituted hydroxymethylene group at the position α to the lactam carbonyl group  
β-Lactams having a substituted hydroxymethylene group at the position α to the lactam carbonyl group are prepared by reaction of an α-halo-β-lactam with zinc or zinc amalgam in an anhydrous...
4267321 Cephalosporin derivatives  
Novel Cephalosporin C derivatives, their production and their use in isolating Cephalosporin C from culture filtrates for subsequent conversion to 7-aminocephalosporanic acid.
4264595 7-[2-(2-Imino-4-thiazolin -4-yl)-2-(syn)-hydroxy-iminoacetamido]-cephalosporins  
Disclosed are 2-(syn)-hydroxyimino-acetamide derivatives of the formula: ##STR1## wherein Y is hydrogen, hydroxyl, an acyloxy, carbamoyloxy, a quaternary ammonium or a nitrogen-containing...
4260746 Chemical intermediates useful to prepare cephalosporins  
7α-Methoxy-7β-acylamino cephalosporins are prepared from 7β-acylamino cephalosporins through formation of a ketenimine by the action of an acid halide, formation of an addition reaction adduct...
4260823 α-Acetylenic derivatives of α-amino acids  
Novel acetylenic derivatives of α-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is...
4254029 Process for preparing β-lactam antibiotics  
Compounds of formula (I): ##STR1## [in which: Z represents a group of formula ##STR2## R represents a hydrogen atom, a 1-pyridyl group or a group of formula --YR' (in which: R' represents an alkyl...
4252973 Process for chemically removing the acyl sidechain from cephalosporins and penicillins  
A process for removing the acyl sidechain from penicillins and cephalosporins which comprises chlorinating the acyl compound and treating the resulting iminochloride with an o-aminothiophenol to...
4251657 Method for removing protective groups  
A halogenoacetyl group is removed from a halogenoacetyl amino compound in a short period of reaction time by reacting the halogenoacetyl amino compound with an N-substituted dithiocarbamic acid or...
4250307 Process for the preparation of 7-amino-cephalosporanic acid  
A novel compound selected from the group consisting of the compound of the formula ##STR1## the metal salts, the ammonium salt and the salts with nitrogen bases, a process for the preparation of...
4245088 Novel 3-acyloxymethyl-cephem compounds useful as intermediates for preparing cephalosporin antibiotics  
Novel 3-acyloxymethyl-cephem compounds of the formula: ##STR1## wherein R 1 is hydrogen or an acyl group; W is acetonyl, or a group represented by --X--COOH or --X--OH (X is an organic residue) or...
4237051 Stereospecific production of 6- or 7-carbon-substituted-β-lactams  
Reaction of 6- or 7-diazo-β-lactams with allylic halides in the presence of a catalytic amount of metallic copper or a copper salt affords 6- or 7-carbon-substituted-β-lactams with the desired...
4236002 Cephalosporin derivatives  
New 7-[4-hydroxy-3-(substituted methyl)phenyl]acetamido cephalosporin derivatives are prepared which are useful as antibiotics.
4230644 Halogenating reagents  
Novel halogenating agents are derived from triaryl phosphites and chlorine or bromine. They are useful in converting 7-acylamino-3-hydroxy-3-cephem compounds to 7-acylamino-3-halo-3-cephems and the...
4229363 4-Hydroxy-3-(substitutedmethyl)-benzeneacetic acids  
New 4-hydroxy-3-(substitutedmethyl)benzeneacetic acids have been prepared which are useful as starting materials in the preparation of cephalosporin and penicillin derivatives.
4225706 Polychalcogen ester of cephem compound, process for preparing the same and method for removing the protective group of the same  
A novel ester of a cephem compound having a carboxyl group at the 4-position in the nucleus; a process for preparing the same by reacting a cephem carboxylic acid or its salt with a halogenide; and...
4224442 7-Ureido acetamido substituted cephalosporin antibiotics  
Cephalosporin antibiotics of the formula ##STR1## wherein R is ##STR2## and R" is H, C 1 -C 3 alkyl, allyl, propargyl, C 3 -C 6 cycloalkyl, phenyl, benzyl or furfuryl; R' is H or methyl; or R...
4223132 Selective conversion of benzyl alcohol carboxylates to the free acid form  
A process for preparing free carboxylic acids which comprises treating an optionally substituted benzyl ester with a Lewis acid, preferably in the presence of a cation acceptor, followed by...
4223135 Production of cephalosporins  
In the preferred embodiment of the present invention trimethylsilyl 7-trimethylsilyloxycarbonylaminodecephalosporanate was prepared by bubbling dry carbon dioxide into an anhydrous solution of...
4219477 Penicillin derivatives  
Penicillin and cephalosporin derivatives and non-toxic salts thereof represented by the formula (1), ##STR1## wherein Ar represents a phenyl or heterocyclic group which may be substituted by a...
4218374 Penam derivatives  
A compound of the general formula: ##STR1## wherein R 1 is amino or a conventional, pharmaceutically acceptable acylamino, R 2 is carboxy or a conventionally protected carboxy, X is --S-- or...
4217275 β-Lactam antibiotic esterification process using methoxymethyl methane sulfonate  
Disclosed is an improved process for esterifying carboxylic acids, particularly 3-carboxylic acid groups of penicillins and 4-carboxylic acid groups of cephalosporins, to form methoxymethyl esters....
4217274 Methoxyethoxymethyl esters of penicillins  
β-Methoxyethoxymethyl esters of cephalosporins and penicillins are exemplified by such esters of hetacillin and heta-amoxicillin were synthesized and found to exhibit advantageous biological...
4211702 Process for preparation of penicillin and cephalosporin imino halides  
Penicillin and cephalosporin imino halides are prepared by reacting of 6-acylaminopenicillins or 7-acylamino cephalosporins with a novel chlorinating compound derived from a triaryl phosphite and...
4209616 Syn isomers of cephalosporins having α-hydroximino- or α-acyloxyiminoacylamido groups at position-7  
The invention provides novel antibiotic compounds which are 7β-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6β-acylamidopenam-3-carboxylic acids, and non-toxic...
4208517 Caphalosporin compounds having at position-7 an α-etherified hydroxyiminoarylacetamido group  
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...
4202817 Process for the production of penam and cephem derivatives  
A process for the preparation of penam and cephem derivatives by reacting a phosphite amide of a 6-aminopenicillanic acid or 7-aminocephalosporanic acid with an acyl halide in an aprotic solvent in...
4189574 Cephalosporin derivatives and process  
A novel compound selected from the group consisting of the compound of the formula ##STR1## the metal salts, the ammonium salt and the salts with nitrogen bases, a process for the preparation of...
4187374 7-(β-Aminoacylamino)-3-substituted-3-cephem-4-carboxylic acid derivatives and preparation thereof  
7-[β-Aminoacylamino]-3-substituted-3-cephem-4-carboxylic acid derivatives of the formula: ##STR1## wherein R 1 is hydrogen, lower alkyl, lower alkenyl, aryl or a heterocyclic group, R 2 is...
4183850 Process for preparing 2-acyloxymethylpenams and 3-acyloxycephams  
A process for preparing 2-acyloxymethylpenams and 3-acyloxycephams of the formulae 1 and 2 ##STR1## in which R represents the aliphatic, aromatic, or heterocyclic moiety of an amino-protecting...
4179557 Acylation of 7-aminocephalosporanic acids  
6-Aminoacylamidopenicillanic acid or 7-aminoacylamidocephalosporanic acids are produced in high yields by acylating 6-aminopenicillanic acid or 7-aminocephalosporanic acid with an amino acid, or a...
4178444 Hydrazono derivatives of cephalosporins  
Hydrazono derivatives of cephalosporins of the formula ##STR1## wherein R is phenyl optionally substituted, 2- or 3-thienyl optionally substituted, or 2- or 3-furyl optionally substituted, R 1 is...
4176231 Process for preparing 3-exomethylenecepham sulfoxides  
3-Exomethylenecepham sulfoxides are prepared by the reaction of 3-methyl-3-halocepham sulfoxides with mercuric or mercurous perchlorate.
4175185 Process for preparing cephalosporanic acid derivatives  
A process for preparing a cephalosporanic acid derivative or a 7-acylaminocephalosporanic acid derivative which comprises subjecting an esterifying agent to reaction in liquid sulfur dioxide in the...
4175076 Azetidinone mercury sulfides and process therefor  
Novel azetidinone mercury sulfides are prepared by the reaction of penicillin derived thiazolineazetidinones with a mercuric halide in the presence of an alcohol or glycol. They are useful...
4172198 7-(N-substituted-2-phenylglycinamido)-3-sub stituted-3-cephem-4-carboxylic acid compounds and preparation thereof  
New cephalosporin compounds of the formula: ##STR1## wherein R 1 is hydrogen or hydroxy, R 2 is a substituted alkanoyl group, R 3 is hydrogen, carbamoyloxy, alkanoyloxy or a heterocyclic-thio...