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JPH0346460B2 |
A process for the preparation of acid amides, comprising reacting a carboxylic acid and an amine in the presence of an isonitrile, wherein the isonitrile has at least one hetero-atom in the substituent present in the above-mentioned ison...
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JPH0346474B2 |
NEW MATERIAL:A compound of formula I [X is halogen: Y and Z incorporate to form a group, =NR<5> (R<5> is protected hydroxyl)], its salt or ester. EXAMPLE:Ethyl alpha-ethoxyimino-2-aminothiazol-4-ylacetate hydrobromide. USE:A synthetic in...
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JPH03502933A |
Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: wherein (1) R<3>, R<4>, and R<5>, together with bon...
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JPH03151389A |
NEW MATERIAL: A compound of formula I [X is H or NHR1 (R1 is H or an amino-protecting group); R is (substd.) spiro-fused or bridged bicyclic group optionally having O, N or S]. EXAMPLE: 6β[Z-[2-(2-Aminothiazol4-yl)-3(bicyclo[2,2,1]hept2...
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JPH0342277B2 |
A process for the debromination of 6-monobromo- and 6,6-dibromopenicillanic acid, and various derivatives thereof, by the action of a bisulfite salt. The debrominated compounds produced find various utilities, as beta-lactamase inhibitor...
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JPH0339514B2 |
Compounds of the formula (I) in which R1 represents lower alkyl substituted by hydroxy or by protected hydroxy, R2 represents carboxy or functionally modified carboxy, and R3 represents optionally substituted 3-pyridyl or optionally subs...
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JPH0337556B2 |
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JPH0333158B2 |
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JPH0332556B2 |
NEW MATERIAL:A compound shown by the formula I (R1 and R2 are lower alkyl; R3 is H or methyl), and its salt. EXAMPLE:6-(2-Amino-2-phenylacetamido)penicillanoyloxymethyl 2beta-(4,5-dimethoxycarbonyl-1,2,3-triazol-1-yl)methyl-2alph
a-methy...
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JPH0332557B2 |
NEW MATERIAL:A compound shown by the formula I (R1 is lower alkyl; R2 is H or methyl) and its salt. EXAMPLE:6beta-[ ( Hexahydro-1H-azepin-1-yl )methyleneamino ]-2, 2-dimethylpenam- 3alpha-carbonyloxymethyl 2'beta-(4-ethoxycarbonyl-1,2,3-...
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JPH0332554B2 |
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JPH0331717B2 |
Compounds of the formula wherein R<1> is H or HO; Y and Z are each Cl, Br or I, or Y is H and Z is Cl, Br or I; Q is N3 or NHCO2CH2C6H4R<4> where R<4> is H, Cl, Br, NO2, CH3 or OCH3; a process for their use in production of the valuable ...
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JPH0331716B2 |
There is provided a process for preparing in high yields a 6-[D(-)- alpha-(4-C1-C4-alkyl-2,3-dioxo-1- piperazinocarbonylamino)- phenylacetamido]penicillanic acid, or pharmaceutically acceptable salt thereof, in which a 4-C1-C4-alkyl- 2,3...
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JPH03106827A |
PURPOSE: To obtain a pharmaceutical composition having improved absorption through a mucomembranous tissue, giving a sufficient hypolevel and useful for oral and intestinum rectum administration by containing an antibacterial compound an...
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JPH0329789B2 |
The invention relates to 2-penem-3-carboxylic acid compounds of the formula (I) in which Ra represents an organic radical bonded by a carbon atom to the ring carbon atom, a free, etherified or esterified hydroxy or mercapto group or a ha...
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JPH0329796B2 |
A process for the preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate which comprises reacting 1,1-dioxopenicillanoyloxymethyl 6-phenylacetamidopenicillante or the corresponding phenoxy- acetamidopenicillanate under ...
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JPH0328438B2 |
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JPH0395185A |
NEW MATERIAL:The compound of formula I [R1 is H, lower alkanoyl or lower alkoxycarbonyl; R2 is lower alkyl substituted with 1-3 F atoms; R3 is (substituted) cycloalkylcarbonyloxyalkyl, cycloalkylalkyl-carbonyloxyalkyl, etc.]. EXAMPLE: (5...
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JPH0395156A |
NEW MATERIAL: A compound of formula I (R1 is an amino having antibacterial activity; R2 is H, a lower alkoxy, a lower alkylthio, etc.; R3 is H or an organic group bonded via C, O, S or N; R4 is an electronegative acidic group, or R3 and ...
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JPH0325435B2 |
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JPH0368582A |
NEW MATERIAL: A compd. of formula I, (where R1 = a lower alkyl, an alkoxy, a halogen; n=0, 1 or 2; R2=H, a lower alkyl or an acyl; R3=H, a lower alkyl, an alkoxycarbonyl or optionally a substd. phenyl; A = a saturated heterocycle compose...
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JPH0321543B2 |
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JPH0321033B2 |
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JPH0318638B2 |
Compounds of formula (I): (I) (wherein R1 represents a C1-C4 alkyl or C1-C3 alpha-hydroxyalkyl group; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group or a cycloalkyl group; R3 represents a hydrogen atom or an al...
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JPH0316356B2 |
PURPOSE:A 2-thioxopenam-3-carboxylic derivative is made to react with an alkylating reagent or hydroxy compound and an azo compound to produce the titled compound used as an antibacterial or synthetic intermediate thereof. CONSTITUTION:T...
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JPH0316357B2 |
PURPOSE:The reaction of an azetidin-2-one derivative with a phosphorous triester or phosphorous acid triamide affords the titled compound that is important as a synthetic intermediate of penem-3-carboxylic acids, antibiotics. CONSTITUTIO...
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JPH0314037B2 |
The invention relates to 2-penem-3-carboxylic acid compounds of the formula (I) in which Ra represents an organic radical bonded by a carbon atom to the ring carbon atom, a free, etherified or esterified hydroxy or mercapto group or a ha...
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JPH0312072B2 |
A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula wherein R'' is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylse...
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JPH0310633B2 |
An improved process for making 6,6-diiodopenicillanic acid, an intermediate for preparation of 6-beta-iodopenicillanic acid, a beta-lactamase inhibitor, which comprises diazotizing 6-beta-aminopenicillanic acid in the presence of iodine,...
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JPH0310632B2 |
Novel 1:2 N,N min -dibenzylethylenediamine, N-benzyl-2-phenylethylamine and dibenzylamine salts of penicillanic acid 1,1-dioxide are prepared which are sparingly soluble in water and therefore valuable as slow release (depot) forms of pe...
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JPH0331289A |
NEW MATERIAL: Compounds given by formula I. USE: Remedy for bacterial infections. PROCESS: An iodomethyl derivative of sulbactam, 3,3-dimethyl-7-oxo-4-thia-1- azabicyclo(3,2,0)heptane-2-carboxylic acid, 4,4-dioxide[2S(2α.5α)] is reacte...
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JPH0327386A |
PURPOSE: To obtain the title antibiotic of high purity extremely low in toxity in high yield by acylating an amino group of specific penicillanic acid by an acid halide in the presence of nicotin or the like. CONSTITUTION: An amino group...
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JPH038357B2 |
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JPH0327385A |
NEW MATERIAL: β-lactam (salt) represented by formula I {wherein R1 is a group represented by formula II [wherein X is a (substd.) monocyclic group or a fused polycyclic aromatic group and OH bonded in this case is conjugated with a grou...
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JPH037675B2 |
A process for preparing 2-methyl substituted penems useful as antibiotics agent and/or as intermediates thereof, by reacting an appropriate 1-imido-3,4-disubstituted azetidinone derivative with a trivalent organophosphorus compound in an...
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JPH0320281A |
PURPOSE: To simply obtain a 6-oxopenicillanate which is an intermediate for preparing penicillin derivatives by the ozone treatment of a diazo compound. CONSTITUTION: A diazo compound of formula I (R is a carboxyl protective group) is di...
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JPH0314578A |
NEW MATERIAL: Compounds of formula I {Q is formula II [A1 is N or CR7 (R7 is H, a halogen, alkyl, etc.); A2 is N or CR2 (R2 is H or a halogen); A3 is N or CH; R1 is H or R15 (R15 is an alkyl, carbon ring, etc.); R3 is H, a halo gen, etc....
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JPH034078B2 |
Preparation of penicillanic acid 1,1-dioxide-and derivatives thereof by debromination of 6-alpha-bromo- and/or 6,6-dibromopenicillanic acid 1,1-dioxides. The debromination is effected in a water-containing medium by reduction with zinc i...
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JPH032157B2 |
A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula wherein R'' is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylse...
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JPH03395B2 |
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JPH03396B2 |
Penems I (R=H, lower alkyl, 2,2,2-trichloroalkyl, benzyl, acetonyl, p-nitrobenzyl, p-methoxybenzyl, Ph, p-nitro-Ph, benzhydryl, acetoxymethyl, Me-CH-OCO2Et, CH2NHCOR2; R2=C1-C5 alkyl, aryl; Z=H, halo, OH, amino, carbamoyloxy, mercapto, p...
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JPH0261942B2 |
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JPH0261478B2 |
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JPH0261470B2 |
A process for producing a brominated 1,3-dioxolen-2-one of the following general formula (I) (I) wherein R1 represents a hydrogen atom, a methyl group, or an aryl group, and R2 represents a hydrogen atom, or R1 and R2 may be bonded toget...
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JPH02306978A |
PURPOSE: To obtain the subject compd. having antibiotic action characteristics in the vicinity of room temp. within a short reaction time in high yield by using a specific azetizinone deriv. as a raw material to react the same with a tri...
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JPH0258266B2 |
The present invention relates to a novel process for the preparation of 7 beta -amino-3- or -2-cephem-3-ol-4-carboxylic acid compound of the formula IA or the formula IB in which R@ denotes hydrogen or an amino protective group R@, R@ re...
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JPH0258271B2 |
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JPH0257063B2 |
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JPH0253434B2 |
The present invention relates to a novel process for the preparation of 7 beta -amino-3- or -2-cephem-3-ol-4-carboxylic acid compound of the formula IA or the formula IB in which R@ denotes hydrogen or an amino protective group R@, R@ re...
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JPH02275885A |
NEW MATERIAL: A compds. being an aminocarboxylic acid deriv. containing a (cyclo)alkylideneammonio group as N-terminal group represented by the formula (wherein X- is an anion from an acid HX, and R1 and R2 are a 1-16C alkyl or form a cy...
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