Abstract: A process for the preparation of a 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester of formula (Ib), in which R1, R2, R3 and R4 are identical or different and are each a C1-6-alkyl. A 2-[-1-amino-1-(4-flourophenyl)methylene]-4-alkyl-3-oxo-alkanoic acid ester of formula (IIIb), in which R3 and R4 have the above-mentioned meanings, is reacted with an N-cyano-N-alkylalkanesulfonamide, optionally isolated or prepares in situ, of formula (IVb), in which R1 and R2 have the above-mentioned meanings, to give the final product of formula (Ib).
Abstract: A method for producing cyanoacetic acid esters of general formula (I):
wherein R represents on optionally substituted linear or branched C1-8 alkyl group or an aryl C1-4 alkyl group. According to the method, an alkoxypropionitrile of the general formula (II):
wherein R is defined above, is oxidized to form the desired product in the presence of a catalyst, based on lead or on one of the transition metals, using oxygen or an oxygen-forming reagent.
Abstract: A method for producing &agr;-dicarbonyl compounds of formula (I):
wherein R1 and R2, independently of each other, mean C1-6-alkyl. In the method, an &agr;,&bgr;-unsaturated ketone of formula (II):
wherein R1 and R2 have the meaning above and R3 and R4, independently of each other, mean hydrogen, C1-6-alkyl or di-C1-6-alkylamino, is reacted with ozone in the absence of a catalyst and the resultant ozonide is treated reductively.
Abstract: The invention relates to a novel method for producing robenidine and salts thereof of the general formula
wherein X denotes a halogen atom. The method uses hydrazine hydrate and a cyano compound YCN as the starting materials, which are first reacted to projuce a diaminoguanidine of the general formula
wherein Y denotes a halogen atom or tosyl. This diaminoguanidine is then converted directly, without isolation, by reacting with a p-halobenzaldehyde of the general formula IV to produce the robenidine and salts thereof of general formula I.
Abstract: A method for producing alkoxy malonic acid dinitrites of general formula (I),
wherein R1 means C1-6-alkyl or halogen-substituted C1-6-alkyl. The method involves converting the corresponding alkoxy malonic acid diamides of general formula (II),
wherein R1 has the aforementioned meaning, by means of a dehydrating agent. The intermediate products of general formula (III),
whereby the products are formed during dehydration.
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
January 6, 2004
Assignee:
Lonza AG
Inventors:
Johannes Bartek, Rudolf Fuchs, Stefan Hildbrand
Abstract: The present invention is directed to a composition for inhibiting microbial growth, which includes a biocide (other than a triamine) and a triamine. The biocide is an oxidizing biocide, a non-oxidizing biocide, or a combination thereof. This composition is particularly effective at preventing the growth of various microorganisms in aqueous solutions, such as industrial waters. The present invention also relates to a method of controlling the growth of microorganisms in an aqueous composition by adding the composition of the present invention to the solution.
Type:
Application
Filed:
January 22, 2003
Publication date:
December 11, 2003
Applicants:
Lonza Inc., Lonza AG
Inventors:
Michael Ludensky, Christopher Hill, Florian Christof Albrecht Lichtenberg
Abstract: Dicyanatochalcones of general formula:
wherein R1 to R8, independent of one another, represent hydrogen, C1-4-alkyl, C1-4-alkoxy or halogen. The compounds can be produced from corresponding dicyanatochalcones by reacting them with chlorine cyanide or bromine cyanide and with a tertiary amine. The compounds are suited for producing polytriazine resins exhibiting good mechanical properties, a low dielectric constant and a good behavior in fire.
Type:
Grant
Filed:
May 29, 2002
Date of Patent:
November 25, 2003
Assignee:
Lonza AG
Inventors:
Sajal Das, Ulrich Daum, Marion Fengler-Veith, Pascal Willa
Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula:
in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.
Abstract: Disinfectants having N,N-bis(3-aminopropyl)octlyamine as the active substance. The disinfectants are characterized by good activity also against mycobacteria, low efficiency loss under protein load and little foaming. The disinfectants are particularly useful for disinfecting surfaces, containers and pipelines, for instance, in the food industry, and for disinfecting instruments, especially automatic instrument disinfection at low temperatures.
Type:
Grant
Filed:
December 26, 2001
Date of Patent:
August 26, 2003
Assignee:
Lonza AG
Inventors:
Florian Lichtenberg, Michael Lützeler, Volker Ranft
Abstract: The invention relates to a novel method for the preparation of optically active 3,3,3-trifluoromethyl-2-alkyl propionic acid derivatives of the general formulae (I) and (II), in which R is ethyl or methyl and X is OH or NH2, provided that if R is methyl X≠—OH. The method comprises the reaction of a racemic propionic acid amide of the general formula (III) either by means of microorganisms which are able to use the propionic acid amide in the form of the racemate or one of its optically active isomers as the only nitrogen source or by means of a polypeptide with amidohydrolase activity which is able to hydrolyze the propionic acid amide. The invention also relates to new optically active representatives of this category of compounds.
Abstract: The process for preparing 1-(6-methylpyridin-3-yl)-2-[(4-methlsulfonyl)-phenyl]ethanone of the formula I:
In a first step, 4-(methylthio)phenylacetonitrile is condensed with a 6-methylnicotinic ester to give 3-[2-(4-(methlthio)phenyl)-2-cyanoacetyl](6-methyl)pyridine of the formula II:
In a second step, the compound of formula II is hydrolyzed and decarboxylated under acidic conditions using a mixture of acetic acid and a mineral acid, to give 3-[2-(4-(methylthio)phenyl)acetyl](6-methyl)pyridine of the formula III:
Finally, in a last step, the compound of formula III is oxidized to give the end product.
Abstract: A five-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-methylsulfonyl)phenyl]ethanone of formula (I):
The process involves the following steps: (a) 4-(methylthio)benzyl alcohol is converted into 4-(methylthio)benzyl chloride; (b) 4-(methylthio)benzyl chloride is converted with an alkali metal cyanide into 4-(methylthio)phenylacetonitrile; (c) 4-(methylthio)phenylacetonitrile is condensed with a 6-methyinicotinic ester to give 3-[2-(2-(methylthio)phenyl)-2-cyanoacetyl](6-methyl)pyridine; (d) 3-[2-(4-(methylthio)phenyl-2-cyanoacetyl](6-methyl)pyridine is hydrolyzed and decarboxylated under acidic conditions to give 3-[2-(4-(methylthio)-phenyl)acetyl](6-methyl)pyridine is hydrolyzed and decarboxylated under acidic conditions to give 3-[2-(4-(methylthio)phenyl)acetyl(6-methyl)pyridine; and (e) 3-[2(4-(methylthio)phenyl)acetyl](6-methyl)pyridine is oxidized to give the end product.
Abstract: The invention discloses a new method for producing enantiomer-enriched 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivatives of the general formulae (I) and (II) in which R1 is hydrogen or a possibly substituted C1-8 alkyl radical, aryl radical or cycloalkyl radical and R2 is acyl.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
February 25, 2003
Assignee:
Lonza AG
Inventors:
Walter Brieden, Kay-Sara Etter, Michael Petersen
Abstract: Microcellular rigid foams with a matrix consisting of cross-linked duromers, especially of polytriazine resins, and with an apparent density of 20 to 95 percent of the density of the compact matrix material. The rigid foams are highly stable and highly temperature resistant and are suitable for use, e.g., as material for aircraft lining.
Abstract: A method for producing 6,6-dialkoxy-5-hydroxy-3-oxo-hexanoic acid esters of general formula (I), wherein the dianion of an acetoacetic acid alkyl ester is reacted with an aldehyde. The 6,6-dialkoxy-5-hydroxy-3-oxo-hexanoic acid esters of general formula (I) are important synthesis building blocks for producing HMG-CoA-reductase-inhibitors.
Abstract: A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.
Abstract: Solvent-free coating materials and treating agents used as water-based wood or material protective agents containing emulsifiable binding agents, quaternary ammonium compounds and optional additional active agents. The wood or material protective agents are non-flammable and enable a uniform distribution of the binding agent and the quaternary ammonium compounds in the substrates. As a result, the quaternary ammonium compounds function as a dissolving mediator for the binding agents which are dispersed in water without opacifying effects and are used as a biocide. The agents can additionally absorb water-insoluble organic biocides without impairing the homogeneity or stability of the formulation of the homogeneity of the distribution in the substrate.
Abstract: The invention relates to a novel process for the preparation of an aminoalcohol of the formula
racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)— or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae
In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula
to give (1S,4R)— or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae
and then cyclized to give the end compounds.
Type:
Grant
Filed:
January 30, 2001
Date of Patent:
September 10, 2002
Assignee:
Lonza AG
Inventors:
Walter Brieden, Josef Schröer, Christine Bernegger-Egli, Eva Maria Urban, Michael Petersen, Jean-Paul Roduit, Katja Berchtold, Holger Breitbach
Abstract: A novel biotechnological process for the preparation of nitriles, starting from amides, is described. Microorganisms of the genus Amycolatopsis, Actinomadura or Rhodococcus are employed for this process.