Abstract: A process for the purification of alkyl alkylacetoacetates of the general formula: ##STR1## in which R.sup.1 is a C.sub.1 -C.sub.10 -alkyl group and R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group. In the process, an alkyl alkylacetoacetate which contains an alkyl alkenylacetoacetate of the general formula: ##STR2## in which R.sup.1 and R.sup.2 have the above-stated meaning, and/or further by-products as an impurity, is converted with an ester of the general formula: ##STR3## in which R.sup.2 has the above-stated meaning, in the presence of a base, into an intermediate which is separated off.
Abstract: Microorganisms of interest are capable of utilizing .alpha.-imino carboxamides, in the form of the racemate or of its optically active isomers, of the general formula ##STR1## wherein A together with --NH-- and --CH-- is an optionally substituted 5- or 6-membered saturated heterocyclic ring, as sole nitrogen source, and converting (RS)-.alpha.-imino carboxamides of Formula I into an S-.alpha.-imino carboxylic acid of the general formula ##STR2## These microorganisms are useful also for biconversion of an (RS)-.alpha.-imino carboxamide of Formula I into an S-.alpha.-imino carboxylic acid.
Type:
Grant
Filed:
March 12, 1996
Date of Patent:
June 16, 1998
Assignee:
Lonza AG
Inventors:
Andreas Kiener, Jean-Paul Roduit, Jorg Kohr, Nicholas Shaw
Abstract: Disclosed is a novel method of producing optically active metallocenyl phosphines of the general formula shown In the formula (Ia) (Ib), M represents iron, ruthenium or nickel; R.sup.1 and R.sup.1' both represent C.sub.1 -C.sub.4 alkyl groups; R.sup.2 and R.sup.3 each represent independently of each other either hydrogen or a C.sub.1 -C.sub.4 alkyl group, or, together with the nitrogen atom, form a five- or six member saturated heterocyclic ring which may optionally contain further heteroatoms; R.sup.4 and R.sup.5 each represent independently of each other a C.sub.1 -C.sub.4 alkyl group (for example) or an aryl group which is optionally substituted with one or more methyl or methoxy groups or with one or more fluorine atoms.
Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formammide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylamino-methylene)pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene)pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.
Abstract: Optically active 3-quinuclidinol is obtained by the asymmetric hydrogenation of 3-quinuclidinone, its Lewis acid adducts or its tertiary or quaternary salts, for example, 1-(diphenylmethyl)-3-oxoquinuclidinium bromide. Rhodium/chiral diphosphine complexes with a metallocene structure are preferably used as catalysts. Optically active 3-quinuclidinol is a synthetic building block for pharmaceutical active substances (M.sub.1 receptor agonists).
Abstract: The 4,4'-methylene-bis-(3-chloro-2,6-dialkylphenylisocyanates) of the general formula ##STR1## are new polyisocyanates for the production of PU systems with high chemical stability and good thermal stability.
Abstract: A process for preparing nicotinamide, wherein, in the first stage, 2-methyl-1,5-diaminopentane is catalytically converted into 3-picoline, then the 3-picoline is converted via an ammonoxidation into 3-cyanopyridine and, finally, the 3-cyanopyridine is converted microbiologically into the nicotinamide.
Type:
Grant
Filed:
October 31, 1996
Date of Patent:
February 17, 1998
Assignee:
Lonza AG
Inventors:
Josef Heveling, Erich Armbruster, Lukas Utiger, Markus Rohner, Hans-Rudolf Dettwiler, Roderick J. Chuck
Abstract: A novel process for the preparation of a 2-alkoxy-6-(trifluoromethyl)pyrimidin-4-ol of the general formula: ##STR1## in which R is a C.sub.1 -C.sub.8 -alkyl group. In the process, cyanamide is reacted with the appropriate alcohol in the presence of hydrogen chloride to give the corresponding alkoxyisourea hydrochloride, which is then converted with ethyl trifluoroacetoacetate in the presence of an alkali metal hydroxide, which is in water, to the end product of the formula I.
Abstract: 4-Oxoimidazolinium salts of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 independently of one another are C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.3-7 -cycloalkyl or optionally substituted aryl, arylalkyl, heteroaryl or heteroarylalkyl, or R.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, form a three-membered to seven-membered saturated or unsaturated carbocyclic or heterocyclic ring, R.sup.3 is a C.sub.1-10 -alkyl group, C.sub.1-10 -alkenyl group, C.sub.3-7 -cycloalkyl group, aryl group, arylalkyl group or heteroaryl group, and A.sup.-- is an anion of a strong acid, are prepared by the cyclization of an .alpha.-acylaminonitrile in a nonaqueous solvent, in the presence of a lower alcohol and a strong acid. The compounds are intermediates for pharmaceutical active substances, for example, angiotensin II antagonists.
Abstract: Tertiary diamines having two saturated heterocyclic rings joined by an aliphatic carbon chain, of the general formula ##STR1## in which each A is a two- to four-membered aliphatic carbon chain substituted if desired by one or more C.sub.1 -C.sub.4 -alkyl groups, are prepared in one stage by catalytic hydrogenation of the corresponding dinitriles of the general formulaN.tbd.C--A--C.tbd.N IIThe diamines preparable in accordance with the invention are particularly suitable as catalysts for the production of polyurethanes.
Type:
Grant
Filed:
January 30, 1997
Date of Patent:
December 16, 1997
Assignee:
Lonza AG
Inventors:
Josef Heveling, Andreas Gerhard, Ulrich Daum
Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichloropyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide.
Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylamino-methylene) pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene) pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.
Abstract: Microorganisms of interest are capable of utilizing .alpha.-imino carboxamides, in the form of the racemate or of its optically active isomers, of the general formula ##STR1## wherein A together with --NH-- and --CH-- is an optionally substituted 5- or 6-membered saturated heterocyclic ring, as sole nitrogen source, and converting (RS)-.alpha.-imino carboximides of Formula I into an S-.alpha.-amino carboxylic acid of the general formula ##STR2## These microorganisms are useful also for biconversion of an (RS)-.alpha.-imino carboxamide of Formula I into an S-.alpha.-amino carboxylic acid.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 22, 1997
Assignee:
Lonza AG
Inventors:
Andreas Kiener, Jean-Paul Roduit, J org Kohr, Nicholas Shaw
Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formammide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylaminomethylene)pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene)pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.