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WO/2003/047740A2 |
Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr ,β−unsaturated ketones. The catalysts are chiral imidazolidinone compounds having the structure of formula (IIA): or (IIB): or are acid a...
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WO/2003/047581A1 |
The invention provides compounds of formula (I) wherein m, n, A, R, R', R', R¿o?, X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g. nerv...
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WO/2003/045921A1 |
The present invention relates to a compound of the formula (I) wherein R?1¿ is optionally substituted aryl; R?2¿ is optionally substituted aryl, optionally substituted heteroaryl, optionally substituted lower cycloalkyl, optionally sub...
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WO/2003/031393A2 |
The invention relates to compounds of the general formula (I), wherein Ar¿1?, Ar¿2?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8?, W, X, a and b have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredien...
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WO/2003/029190A1 |
Processes for the efficient production of chiral amino nitriles are disclosed. Generally, the processes include the esterification of the alcohol of an amino protected alcohol followed by nucleophilic substitution of the ester with a cya...
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WO/2003/029200A2 |
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6?, R¿8?, R¿9? and X aredefined herein. The compoundsare useful for treating autoi...
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WO/2003/024591A1 |
The invention relates to a process for the preparation of an active alumina catalyst impregnated with a base, which is chosen from alkali or alkaline earth metals and its synthetic applications. The catalyst has been used for the protect...
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WO/2003/020684A1 |
The present invention describes immobilized haloenamine reagents, immobilized tertiary amides, methods for their preparation, and methods of use.
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WO/2003/018552A2 |
The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of -haloenamine reagents, which may o...
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WO/2003/011799A1 |
One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing cataly...
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WO/2003/010134A1 |
Disclosed is a method for the production of 1,2,4-triaminobenzolecarbamic acid esters, characterized by the use of pyro- or polypyrocarbonate. The use of pyro- or polypyrocarbonate results in increased yields and increased purity of said...
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WO/2003/010089A1 |
The invention relates to a method for obtaining an ammonium carbamate solution from a gas mixture that contains more than 40 wt.% NH3, less than 50 wt.% CO2 and less than 40 wt.% H2O and has a pressure between 0.1 MPa and 4 MPa, comprisi...
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WO/2003/002509A1 |
A method is provided for processing a solution having optical isomers .to obtain a (2R,38) target isomer: wherein P¿1? is H or a hydroxyl protecting group, R¿1? is H, an alkyl group, an olefinic group or an aromatic group, and R¿2? is...
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WO/2003/002512A1 |
A process for efficiently producing a hydroxyamino acid derivative, especially an optically active isomer thereof. The process, which is for producing a hydroxyamino acid derivative represented by the formula (I): (I) or a salt thereof, ...
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WO/2002/102764A2 |
The invention relates to a method for producing chiral amino acid derivatives, characterised in that free carboxylic acid groups in an amino acid derivative are first converted into nitro ketones, and said nitro ketones are then converte...
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WO/2002/100849A2 |
Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases a...
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WO/2002/098843A2 |
The present invention relates to discodermolidate acid salts of formula (I) where R is as defined herein, pharmaceutical compositions containing said salts, the use of said salts alone or in combination with other therapeutic agents in t...
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WO/2002/096853A1 |
An aromatic aldehyde derivative represented by the general formula (1): Ar−CHO (1) (wherein Ar represents an aromatic group) is reacted with trichlorosilane and a carbamate represented by the general formula (2): NH2COOR (2) (wherein R...
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WO/2002/090322A1 |
This invention relates to a process for the preparation of alkyl-N-(3-dimethylamino)alkylcarbamates by reacting an alkyl-chloroformate in an alcohol.
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WO/2002/088050A2 |
The process disclosed herein satisfies the need in the art for an industrially viable oxidative carbonylation catalytic system, and is capable of producing carbamates at a significantly higher rate than those processes reported in journa...
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WO/2002/088085A2 |
This invention relates to methods for preparing certain cholesteryl ester transfer protein (CETP) inhibitors IA or IB and intermediates related thereto.
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WO/2002/085877A2 |
Disclosed are intermediates and processes for preparing epoxides of the formula (1): where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the product...
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WO/2002/085838A1 |
The present invention relaters to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the ...
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WO/2002/083627A2 |
The invention relates to the novel biphenyl derivatives of the general formula (I), wherein R1, R1', R1'', R2 and n are defined as in claim 1. The invention also relates to the stereoisomers and the physiologically acceptable salts or so...
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WO/2002/083626A2 |
The invention relates to alkyl and/or alkenyl glycerol carbamates obtained by reacting glycerol, diglycerol and/or polyglycerol carbonate with a primary and/or secondary amine of formula (I): HNR?1¿R?2¿. In said formula, R?1¿ represen...
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WO/2002/079148A2 |
The present invention provides a more economical method of producing multifunctional carbonate resins. It overcomes the disadvantage of using relatively expensive starting material, such as polyglycidyl ethers, that have traditionally be...
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WO/2002/060893A1 |
The present invention includes a method for carbamoylating an alcohol with sodium cyanate in the presence of methanesulfonic acid. The reaction can be conducted under anhydrous conditions. This method is suitable for carbamoylating a mol...
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WO/2002/060862A1 |
This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X¿2? is a halo group, and is -F, -Cl, -Br, or -I; n is a...
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WO/2002/055499A1 |
Novel intermediates (X and VIII) and the use thereof in a process for the preparation of pyridinoline(I).
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WO/2002/055483A1 |
An anilide is reacted with an acylating agent by using as a catalyst a tri(perfluoroalkane sulfonate) compound of any of the elements belonging to the groups 3 to 5 and the groups 13 to 15 in the periods 4 to 6 of the periodic and thus t...
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WO/2002/055486A2 |
The invention relates to novel triazene compounds, the use thereof and novel alkylation methods. Said triazene compounds have the general formula, X-Y-Z-N=N-NH-R, where X = an insoluble support material, Y = an atom, or group of atoms, f...
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WO/2002/051781A1 |
A process for producing an optically active halohydrin compound, characterized by subjecting an $g(a)-haloketone compound to asymmetric hydrogen transfer reduction in the presence of a Group 9 transition metal compound having an optional...
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WO/2002/048095A1 |
A process for efficiently producing a-aminohalomethyl ketone derivatives appropriate for industrial production which is characterized by subjecting a-aminodihalomethyl ketone derivatives to catalytic reduction.
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WO/2002/044136A1 |
A process for purifying N-protected-ß-amino alcohols (such as (2R, 3S)- or (2S, 3R)-3-t-butoxycarbonylamino-1 halo -2-hydroxy-4-phenylbutane) either by adding water to a solution of such an alcohol in a polar organic solvent to crystall...
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WO/2002/042348A2 |
The present invention is directed to a low viscosity carboxyl-containing polyol composition having a viscosity in the range of about 3,000-100,000 centipoise, and having an oligomer content of less than 30 mg KOH/g. Preferably, the carbo...
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WO/2002/036544A1 |
A method of resolving optical isomers which comprises mixing in an aqueous solution an amino acid derivative in the form of a mixture of D- and L-isomers (for example, N-(tert-butoxycarbonyl)-DL-alanine) with a hydrophilic compound isome...
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WO/2002/034725A1 |
The invention relates to novel substituted phenyluracils of formula (I) wherein R?1¿ represents hydrogen, amino or respectively optionally substituted alkyl, alkenyl or alkinyl, R?2¿ represents cyano, carboxy, carbamoyl, thiocarbamoyl ...
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WO/2002/034698A2 |
A phosgene-free method for preparing a carbamate from a compound containing an amine group involves reacting the compound with an alkylating agent in the presence of carbon dioxide and cesium carbonate. A reaction can take place under st...
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WO/2002/030565A1 |
The invention concerns the use as catalyst for transforming carbamates of compounds corresponding to the general formula (I): -Sn (X) (X") wherein: X" is selected among chloride, bromide, iodide, thiocyanate radicals, sulphonate radicals...
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WO/2002/031014A1 |
The invention concerns a novel catalyst for forming urethanes. Said catalyst is characterised by the general formula: MY¿3 q?[Z]¿q?, wherein: Z is the radical corresponding to the anion of a super acid whereof the Hamett constant is at...
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WO/2002/026705A2 |
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one s...
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WO/2002/026750A2 |
Disclosed are substantially enantiomerically pure bis-phosphine compounds comprising a substantially enantiomerically pure chiral backbone linking two phosphine residues wherein one of the phosphine residues has three phosphorus-carbon b...
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WO/2002/026700A1 |
A method of preparing hydroxyalkylcarbamates from six-membered cyclic carbonates. The method involves reacting a six-membered cyclic carbonate with anhydrous ammonia or aqueous ammonium hydroxide. The present invention also provides for ...
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WO2001096282B1 |
The invention relates to a method for producing amides or esters from carboxylic acids and from an amine constituent or alcohol constituent in the presence of a 1,3,5-triazine and optionally in the presence of an organic solvent and of a...
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WO/2002/026695A2 |
Disclosed are processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives by the hydrogenation of certain enamides in the presence of a catalyst comprising a transition metal and a substantially enantiomeric...
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WO/2002/024671A1 |
The invention concerns a process for the production of optically active epoxides useful as pharmaceutical intermediates, particularly in the field of HIV protease inhibitors. The optically active epoxides are produced in commercially acc...
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WO/2002/022549A1 |
A process which comprises reacting a 2- or 4-nitro- benzenesulfonamide with an alkali metal alkoxide to remove the nitrobenzenesulfonyl group and thereby obtain an amine corresponding to the amide, and, if necessary, reacting this amine ...
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WO/2002/020469A1 |
The present invention relates to a substrate useful to bio-chips comprising a molecular layer having low surface density of amines, and it provides a compound of Chemical Formula (1) represented by N-CBZ-[1]amine-[9]acid having a carboxy...
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WO/2002/020472A1 |
The invention relates to substituted phenylcyclohexane carboxylic acid amides of formula (I), a method for the production thereof and the use thereof in medicaments, especially in the prevention and/or treatment of cardiovascular diseases.
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WO/2002/020470A1 |
The invention aims at providing processes for the production of amino acid derivatives of the general formula (I) and t-butoxycarbonylaminoethylamine being an intermediate for the production of the derivatives (I), which can attain high ...
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