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WO/1999/018947A1 |
A process to make the S(+)mandelic acid salt of $i(N)-methyl-3$i(R)-hydroxy-3-phenylpropylamine comprising reacting $i(N)-methyl-3($i(R,S))-hydroxy-3-phenylpropylamine with S(+)mandelic acid is described and claimed. Also described and c...
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WO/1999/018057A1 |
One aspect of the present invention relates to novel reaction conditions that allow the efficient synthesis of diaryl ethers from arenes bearing a leaving group and arenols under relatively mild conditions. Another aspect of the present ...
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WO/1999/016746A1 |
Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.
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WO/1999/012888A1 |
The invention relates to a method for producing aryloligoamines, characterised in that an amine is reacted with an activated aromatic and a base within a temperature range from 0 and 150 °C in the presence of a palladium constituent and...
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WO/1999/011600A1 |
A process for enhancing the purity of 2R-[1-hydroxy- 1-trifluoromethyl- 3-cyclopropylpropyn-2-yl] -4-chloroaniline comprising the formation of an acid addition salt which is capable of rejecting the racemate in the selected organic solvent.
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WO/1999/005088A1 |
A method of preparing a first geometric isomer of tamoxifen or an analogue comprises allowing the first isomer to crystallise in hexanol and the product thereof to crystallise in methanol and then derivatising the product of the methanol...
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WO/1999/005089A1 |
The invention concerns novel N-alkyl-hydroxybenzylamines of formula (I) in which: R¿1? and R¿2?, which are identical or different, represent a hydrogen atom or a monohydroxylated or polyhydroxylated C¿1?-C¿8? alkyl radical, provided ...
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WO/1999/003820A1 |
Cis-Tramadol hydrochloride is prepared by forming a Mannich hydrochloride, liberating the Mannich base, reacting the Mannich base with a Grignard reagent to form a base hydrate of cis-Tramadol which is used to form pure cis-Tramadol hydr...
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WO/1999/001418A1 |
The invention relates to a novel method for aminating mononuclear aromatic compounds and polynuclear compounds containing at least one aromatic ring. The inventive method enables simple separation of the aminated mononuclear aromatic com...
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WO/1999/001419A1 |
A process for producing 2-aminomalonic acid derivatives of general formula (1) (wherein A is linear or branched alkylene having 1 to 10 carbon atoms; R?1¿ is linear or branched alkyl having 2 to 20 carbon atoms; R?2¿ and R?3¿ may be t...
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WO/1999/001417A1 |
The present invention provides optically pure (S) 2-methylamino-2-phenyl-$i(n)-butyl 3,4,5-trimethoxybenzoate for use in the treatment of chronic pain, and having Formula (I). The present invention also provides methods of using the comp...
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WO/1999/001376A1 |
The present invention provides a method and composition regeneration of an aminal that has previously been reacted with a sulfide selected from hydrogen sulfide and mercaptans. The method includes contacting a scavenging mixture which in...
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WO/1999/001420A1 |
A process for the preparation of 2-aminomalonic acid derivatives of general formula (1), characterized by deacylating compounds of general formula (2), halogenating the resulting compounds, reacting the resulting halogenated compounds wi...
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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/1998/057921A1 |
The invention concerns a method for preparing a compound of formula (I) in which: R?1¿ represents a C¿1?-C¿10? alkyl group, linear or branched, an aralkyl group in which the alkyl part is linear and comprises 1 to 3 carbon atoms and t...
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WO/1998/056753A1 |
Oxidation of secondary amines with hydrogen peroxide and sodium tungstate is reported to give good yields of nitrones. However, when using dimethylamine in this manner, a considerable amount of N,N-dimethylformamide was produced as a co-...
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WO/1998/054121A1 |
The invention concerns a method for preparing a compound of formula (I) comprising the following steps consisting in: a) optionally reacting a compound of general formula (II) with a nitrating reagent; b) reducing the compound obtained a...
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WO/1998/052907A1 |
The present invention relates to biodegradable softener compounds of the formula (1): [(R)�4-m?-N(?+�)-[(CH�2?)�n?-Y-R?1�]�m?] X(?-�) with an acid value of no more than 6.5. A process for making said compound is also provid...
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WO/1998/051676A1 |
An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihy
dro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addit...
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WO/1998/045278A1 |
The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihy
dro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HI...
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WO/1998/045248A1 |
Process for the preparation of cericlamine which consists: i) in arylating methacrylic acid with the diazonium chloride of 3,4-dichloroaniline, to obtain (+/-)2-chloro-3-(3,4-dichlorophenyl)-2-methylpropionic acid, ii) in aminating the a...
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WO/1998/045247A1 |
A process for the preparation of 3-amino-1,2-propanediol, commonly known as isoserinol, having an organic impurities content lower than 0.1 % and an inorganic impurities content lower than 0.05 %.
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WO/1998/043942A1 |
The invention relates to novel compounds of Formula (I) wherein R?1�, R?2�, R?3�, R?4�, R?5�, R?6�, R?7� and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in ...
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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/1998/038154A1 |
Compounds of formula (II) wherein r is an integer selected from 5, 6 and 7; s is an integer selected from 2 and 3; A is O or a single bond; R'�4?, R'�5? and R'�6?, the same or different, are hydrogen, OH, halogen, nitro, C�1?-Cï¿...
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WO/1998/038155A1 |
Compounds of formula (I) wherein R�1? and R�2? are independently hydrogen or an optionally branched C�1-4? alkyl group; the asterisk marks an asymmetric carbon atom; and the pharmaceutically acceptable salts thereof, useful in card...
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WO/1998/038153A1 |
A process is disclosed for preparing N,N,N',N'-tetra-(2-hydroxyethyl)-ethylenediamine in a solvent. Ethylenediamine is selectively reacted with ethylene oxide in the absence of water in one or several saturated C�3?-C�9?-alcohols at ...
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WO/1998/034905A1 |
The invention provides a process for the production of a 2,3-dihydroxypropylamino compound, said process comprising the reaction steps of: (i) obtaining an allylamino compound; (ii) epoxidizing said allylamino compound to yield an epoxyp...
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WO/1998/033762A1 |
S(-)-amino-6-fluoro-7-methoxytetraline, a process for its preparation and pharmaceutical compositions containing same, active in preventing and treating septic shock, are disclosed.
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WO/1998/032519A1 |
A process is disclosed for the neutralization of amine or alkanolamine heat stable salts with aqueous KOH or with alkali metal base, such as potassium hydroxide, sodium hydroxide, sodium carbonate, potassium carbonate, sodium bicarbonate...
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WO/1998/029402A1 |
Disclosed is a novel intermediate, 3,4-dihydro-6-methyl-4-phenyl-2H-benzopyran-2-ol of formula (IV) and an improved process for the preparation of tolterodine.
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WO/1998/029401A1 |
A method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80 �C, wherein said halomethyl organometallic reagent is form...
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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/1998/024753A1 |
Optically active 1-(substituted phenyl)-2-nitro alcohol derivatives represented by general formula (1) and a process for preparing the same, and 1-(substituted phenyl)-2-amino alcohol derivatives represented by general formula (2) and a ...
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WO/1998/024755A1 |
The present invention relates to a process for the preparation of 2-amino-1,3-propanediol, having a content of organic impurities lower than 0.1 % and inorganic impurities lower than 0.05 %, comprising the following steps: a) formation o...
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WO/1998/023559A1 |
The invention concerns a method for splitting 1-amino-alkan-2-ol compounds of general formula (I) in which R can represent a large variety of alkyl groupings using as splitting agent one of the enantiomers R or S of N-tosyl-leucine.
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WO/1998/022426A1 |
A method for the manufacture of metoprolol wherein the process is performed in water as solvent.
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WO/1998/022427A1 |
Aminohydrofluorides with the general formula (I): R-N(CH�2?CH�2?OH)�2? . HF in which R is a straight-chain hydrocarbon residue with 10 to 20 carbon atoms, have an anti-bacterial and caries-prophylactic effect. They can be prepared ...
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WO/1998/021175A1 |
A method is disclosed for the preparation of optically pure isomes of formeterol, especially the ($i(R,R))- and ($i(S,S))-isomer, by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-...
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WO/1998/020005A1 |
The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive. The...
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WO/1998/017230A2 |
The new compound of Formula (I) and salts thereof possess valuable anxiolytic properties.
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WO/1998/015533A1 |
2,3-dihydroperimidines of formula (I), in which X, m, R?1� and R?2� have the meaning cited in the description, are produced by the reaction of 1-hydroxy-8-aminonaphthalines of formula (II) with carbonyl compounds of the formula (III)...
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WO/1998/015522A2 |
The invention concerns a method for preparing trans-4-(4-aminomethylphenyl) cyclohexanol derivatives of formula (I) in which R�1? and R�2? represent, independently of each other, one C�1-6? alkyl group, linear or branched, one benz...
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WO/1998/014436A1 |
The present invention relates to benzoxazinones of formula I, or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical comp...
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WO/1998/013334A1 |
Provided is a novel process for the preparation of iohexol having improved yields and purity, reduced number of isolated intermediates, and significantly reduced volume of ion-exchange resins required to desalinate the final product.
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WO/1998/012171A1 |
A process for the preparation of 3-amino-2-hydroxy-1-propyl ethers of general formula (4), (wherein R?1� is alkyl, or an aromatic or heterocyclic group; and R?2� and R?3� are each hydrogen or alkyl, or alternatively they together w...
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WO/1998/012172A1 |
The present invention relates to a process for the selective alkylation of intermediates of betaxolol.
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WO/1998/011054A1 |
The invention relates to a process for the preparation of N-methyl-[3-phenyl-3-[4-(trifluoromethyl)-phenoxy]-propyl]-a
mine of the Formula (I) and pharmaceutically acceptable acid addition salts thereof by reaction of N,N-dimethyl-{3-phe...
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WO/1998/011064A1 |
This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to ...
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WO/1998/011053A1 |
The invention concerns a method for preparing an optically active alcohol of formula (I) in which the carbon atom indicated by the symbol * can have the configuration ($i(R)) or ($i(S)) and X represents an amino group not substituted or ...
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