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WO/2000/051968A1 |
The present invention is directed to a method for the preparation of a chiral $g(b)-amino ester of formula (I) or (II), wherein R is lower alkyl; and X and Y are the same or different halogens selected from the group consisting of CI, Br...
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WO/2000/050378A2 |
The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula (I): In Structural Formula (I), R is an amine protecting group, and R?1¿ is an amino acid s...
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WO/2000/050389A1 |
A method of preparing carbamates of the general formula RR'-N-CO¿2?-R'' by reacting an amine with carbon dioxide and an organic electrophile in an anhydrous solvent in the presence of a cesium base, whereby carbamate synthesis is accomp...
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WO/2000/048623A1 |
Disclosed are the novel compounds as growth hormone secretagogues represented by structural Formula (I), wherein R?1¿ is, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, ...
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WO2000011020A9 |
The invention relates to a method and reagent for the synthesis of peptides containing deoxyhypusine, the reagent having formula: (1) wherein: Q1 and Q2 may be the same or different and are amino protective groups, and Q3 is an amino pro...
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WO/2000/044706A1 |
A process which comprises converting a $g(a)-amino acid ester into the corresponding imine to thereby protect the amino group of the ester, reacting the imine with a halomethyllithium to form an N-protected $g(a)-amino halomethyl ketone,...
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WO/2000/043343A2 |
A method for the cross-metathesis of terminal olefins is disclosed. The method describes making disubstituted internal olefin products by contacting a first terminal olefin with another first terminal olefin to form a dimer and then cont...
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WO/2000/043357A1 |
To efficiently isolate (2S,3S)-1-halo-2-hydroxy-3-N-(tert-butoxycarbonyl)amino-4-ph
enylbutanes (1) or (2R,3S)-1-halo-2-hydroxy-3-N-(tert-butoxycarbonyl)amino-4-ph
enylbutanes (2) with excellent qualities, impurities are eliminated from ...
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WO/2000/041476A2 |
Compounds of formula (I) wherein R¿1? is C¿1?-C¿4?-alkyl or cyclopropyl; R¿2? is C¿1?-C¿6?-alkyl, C¿2?-C¿6?-alkenyl, C¿2?-C¿6?-alkinyl; or C¿1?-C¿6?-alkyl substituted by 1 to 5 fluorine atoms; R¿3? is C¿1?-C¿6?-alkyl, C¿1...
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WO/2000/041998A1 |
Propargylether derivatives of formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R¿1? is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R¿2? and R¿3? are each independently hydrogen or...
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WO/2000/041997A1 |
3 process for the preparation of optically active $g(b)-amino alcohols represented by the general formula (2): Ra-C*H(OH)-C*H(Rb)-Rc, [wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, or the like; Rb is on...
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WO/2000/040529A1 |
The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R?7¿)- wherein R?7¿ is hydrogen, hydroxy, C¿1-7?alkoxy, -OR?8¿ or -NR?8¿R?9¿ (wherein R?8¿ is a group -Y?1¿R?10¿ (wherein ...
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WO/2000/035864A1 |
The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the tre...
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WO/2000/027799A1 |
New esters derived from substituted phenyl-cyclohexyl compounds, derived from tramadol, process for obtaining such esters and use of said compounds for the fabrication of a medicament having analgesic properties. These new products havin...
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WO/2000/024704A1 |
A process for producing peptidyl aldehyde derivatives represented by general formula (I), wherein A represents amino acid-origin acyl; and R¿1? and R¿2? are different and one represents hydrogen while the other represents optionally su...
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WO/2000/017157A1 |
The invention relates to novel optically active substituted N-aryl-O-aryloxyalkyl-carbamates of general formula (I) in which Ar?1¿ represents an optionally substituted, monocyclic or bicyclic, carbocyclic or heterocyclic grouping from t...
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WO/2000/014057A1 |
A new method for the production of carbamates the said method comprising reacting a hydroxy containing compound and N-methyl isocyanate at a temperature and a pressure to maintain the compound in the liquid state.
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WO/2000/009463A1 |
The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile, selected from the group consisting of water, alcohols, carboxylic acids, and thiols, an...
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WO/2000/007974A1 |
A 14-acyloxy derivative of mutilin or 19,20-dihydromutilin having a 2-fluoro substituent of structure (a), (b), in which R?1¿ is vinyl or ethyl, and R?a¿.CO.O- is an acyloxy group. The acyloxy group may be HOCH¿2?CO¿2?- or R-X-CH¿2?...
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WO/2000/007976A1 |
A synthesis of fluoxetine is disclosed. The process begins with benzoylacetonitrile, which is reduced, optionally in the presence of a chiral ligand, to produce the corresponding aminoalcohol, and the amine is carbamoylated without isola...
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WO/1999/067192A2 |
This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and $g(a),$g(b)-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds us...
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WO/1999/067228A1 |
This invention is directed to a fluorophenyl resin compound, to methods of its preparation; and to its use in the solid phase synthesis of amides, peptides, hydroxamic acids, amines, urethanes, carbonates carbamates, sulfonamides and $g(...
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WO/1999/062871A1 |
Novel 3-aryl proprionic acid derivatives and analogs, having general formula (I) and stereo- and optical isomers and racemates thereof as well as pharmaceutically acceptable salts, solvates and crystalline forms thereof, process for thei...
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WO/1999/052855A1 |
The present invention relates to a process for preparing chiral (S)-2,3-disubstituted-1-propylamine derivatives and more particularly, to the process for preparing chiral (S)-2,3-disubstituted-1-propylamine derivatives expressed in formu...
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WO/1999/052850A1 |
The present invention relates to an oxidation which converts a primary or secondary alcohol of Formula (II) to an acid or ketone of Formula (I) with periodic acid and a catalytic amount of a chromium reagent.
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WO/1999/052849A1 |
The present invention relates to the oxidation of a primary alcohol of Formula (II) to the carboxylic acid of Formula (I): R?1¿CH¿2?OH$m(7)R?1¿CO¿2?H.
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WO/1999/050234A1 |
Novel urethane compounds which are utilizable as blocked isocyanates, materials for diisocyanates, color developers for thermal recording papers, materials for powder coating materials, etc. They are biscarbamic ester compounds represent...
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WO/1999/050214A1 |
A process comprising subjecting at least one compound containing at least one carbon-carbon double bond or at least one carbon-carbon triple bond, hydrogen and carbon monoxide, to a hydrocarbonylation reaction in supercritical carbon dio...
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WO/1999/047493A1 |
Organic carbamates are prepared by the reaction of organic amines (preferably aromatic polyamines) with heteroatom-substituted alkyl carbonates. Said carbamates can be thermolysed into the corresponding isocyanates.
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WO/1999/038844A1 |
The present invention relates to a method for preparing an N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound of formula (I) wherein R¿a? is (II); R¿aa? is hydrogen, optionally substituted aliphatic or optionally substituted...
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WO/1999/035122A1 |
The invention relates to a method for producing N-(3-amino-4-fluorophenyl)- sulphonamides, N-(3-amino-4-fluorophenyl) carboxylic acid amides and N-(3-amino-4-fluorophenyl) carbamates of general formula (I), wherein A stands for SO¿2?, C...
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WO/1999/021823A1 |
Intermediates having formulas (A) and (B) wherein B?I¿ is -CH¿2?OH or -CH¿2?OR?P¿, and R?P¿ is an alcohol protecting group; a is 1, 2, or 3; T?I¿ is -OH or (C); Q?I¿ is phenyl, naphthyl or heteroaryl having 1-3 substituents; R?a¿...
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WO/1999/006351A1 |
This invention concerns the use of a hydroxylic solvent in the preparation of enaminones from the corresponding amine N-oxides or propargylic amines via the general process outlined above (A).
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WO/1998/058900A1 |
The invention concerns a method for displacing, at least partially, an aniline from its chlorhydrate, characterised in that said aniline is selected among anilines whereof the conjugate acid has a pKa not more than 6 and in that it consi...
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WO/1998/058906A1 |
The invention concerns a method for transforming an aminophenol, characterised in that it consists in a step whereby said aminophenol aniline function is in the form of am anilide function and said phenol is dissolved in a water-repellen...
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WO/1998/055452A1 |
A process for stereoselectively reducing $g(a)-amino haloketone derivatives under mild conditions, which comprises reacting an $g(a)-amino haloketone derivative of general formula (1) with a compound prepared from an organoaluminum compo...
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WO/1998/055450A1 |
Method for the preparation of carbamates by reaction of aromatic amines with organic carbonates in the presence of a metal based catalyst on an inert carrier support.
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WO/1998/055451A1 |
Method for the preparation of carbamates by reaction of amines with organic carbonates in the presence of a metal based catalyst wherein the reaction is carried out under such conditions that a precipitate containing said metal is formed...
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WO/1998/052552A1 |
Disclosed are processes for the preparation of compounds of the formula (I): H�2?N-(CH�2?)�n?-A-(CH�2?)�m?-NH�2?, or (II): H�2?N-(CH�2?)�n?-NH-C(=NR?1�)-NH-(CH�2?)�m?-NHï¿
½2?, wherein n and m are each independent...
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WO/1998/050345A1 |
The reactions of cyclic carbonates, especially 1,3-dioxolan-2-ones, with amines, especially primary amines, are catalyzed by the presence of a base whose conjugate acid has a pKa of about 11 or more. The products are hydroxy urethanes, a...
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WO/1998/046794A1 |
Peptide nucleic acid monomers are provided having chirality in their backbones, as are synthetic methods therefor and peptide nucleic acid oligomers prepared therefrom.
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WO/1998/041489A1 |
An enantiomeric mixture of a chiral amino acid is separated into its respective enantiomers through chromatography on a chiral polysaccharide stationary phase eluting with a mobile phase comprising (i) a liquid lower alkanol and (ii) a c...
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WO/1998/040348A1 |
The present invention relates to a method for producing N-carboxyalkyl-3-fluoro-4-dialkylaminonilines by reacting an ortho-nitrochlorobenzene of formula (1), wherein X stands for Cl or F, with a secondary amine of formula (2) HNR?1�R?2...
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WO/1998/035936A1 |
A process for producing an aryl carbamate of a high purity in a high yield by reacting a diaryl carbonate with an amine compound having one or more hydrogen atoms bonded to the N position in the presence of carboxylic acid(s) of the foll...
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WO/1998/031663A1 |
The invention concerns novel modifications to the compound 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonyl-aminobenzen
e of formula (I). The invention also concerns processes for preparing this compound and its use in pharmaceutical com...
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WO/1998/029376A1 |
This invention is directed to processes for the solid-phase synthesis of aldehydes, ketones, oximes, amines and hydroxamic acid compounds and to polymeric hydroxylamine resin compounds useful therefor.
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WO/1998/027052A1 |
This invention relates to an improved process for the production of known amine compounds of formula (I) which are useful as medicaments, wherein: R?1� and R?2� are independently phenyl or 4-fluorophenyl; R?3� is hydrogen, alkyl Cï...
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WO/1998/024741A2 |
A process for the preparation of carbocyclic stereoisomers of formulae (I), (I'), (IIA'), (IIB'), (VA') and (VB'), including enantiomerically pure (IIA'), (I) and (I') utilising fractional crystallisation of salts formed with a chiral ba...
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WO/1998/022429A1 |
The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.
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WO/1998/018756A1 |
This invention is directed to a method for making an iodopropargyl carbamate in an aqueous reaction medium so as to yield a more pure and stable, e.g., U.V. resistant, product in a high yield, free from environmental hazards posed by usi...
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