Dsm Fine Chemicals Austria Nfg Gmbh & Co. Kg

Amazentis Sa

Actelion Pharmaceuticals Ltd

Newron Pharmaceuticals S.p.a.

Wolfgang Skranc

Irma Wirth

Herbert Mayrhofer

Rudolf Neuhofer

Helmut Schwab

Anton Glieder

George Yiannikouros

Peter Poechlauer

Christopher Goss

Zhixing Shan

Alexander Trofimov

Christopher Rinsch

Michael Stanek

Marcel G Wubbolts

Peter Pöchlauer

Christoph Kratky

Ingrid Dreveny

Christoph Zenzmaier

Manuela Hermann

Micheal Stanek

Felix Spindler

Ralf Koberstein

Gerhard Steinbauer

Zarghun Nazir

Harald Pichler

Christoph Imboden

Peter Pojarliev

Wilhelm Tschebull

Doris Domin

Rodolfo Bona

Matthias Helms

Joannes Kierkels

Andreas Hendrikus Maria De Vries

Gerardus Karel Maria Verzijl

Herfried Griengl

Erhard Bappert

Erwin Waldvogel

Michael Wolberg

Karl Gruber

Maria Andreas Hendrikus De Vries

Matthias Riepl

Martin Fechter

Roland Mueller

Roland Müller

Ruud Luiten

Roland Weis

Jurgen Stichler

Maria Gerardus Karel Verzijl

Ralph Koberstein

Roland Muller

Andreas Hendrikus De Vries

Gerardus Karel Verzijl

Christpoher L Rinsch

Marcel Wubbolts

Methods for preparing a salt of urolithin A and, in turn, urolithin A. Combining in an alkaline aqueous solution a copper-containing catalyst, 2-bromo-5-hydroxybenzoic acid, and resorcinol produces a salt of urolithin A. Urolithin A has been prepared by protonating a salt of the compound.

Process-scale synthesis of urolithin A

The present invention relates to a new process for the production of substituted 2-[2-(phenyl) ethylaminojalkaneamide derivatives of the following formula (I), in particular 2-[2-(3-butoxyphenyl)-ethylamino]-N,N-dimethylacetamide in high yields with very high chemical purity. The invention relates to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof:

Process for the production of substituted 2-[2-(phenyl) ethylaminojalkaneamide derivatives

Disclosed are methods for preparing a salt of urolithin A and, in turn, urolithin A. The methods are advantageous for the large-scale preparation of urolithin A or a pharmaceutically acceptable salt thereof.

Disclosed is a method of preparing a urolithin, or an intermediate or analog thereof, having a dibenzo[b,d]pyran-6-one core. The method is especially advantageous for the large-scale preparation of urolithins or intermediates or analogs thereof. The method may optionally include the preparation of a urolithin, or an intermediate or analog thereof, as a pharmaceutically acceptable salt.

Process-scale synthesis of urolithins

Polypeptide and recombinant protein having esterase activity which exhibit the amino acid sequence SEQ. ID. No. 1 and the use thereof.

Polypeptide having esterase activity and recombinant esterase and use thereof

The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-&#x3b1;-(dimethylamino)-2-(dicyclohexylphosphino)benzyl]-ferrocene as a catalyst. 

Process for the preparation of an enantiomeric trisubstituted 3,4-dihydro-isoquinoline derivative

The present invention relates to the compound of formula 7*acetate (see below), a process for its preparation, and its use 

Trisubstituted 3,4-dihydro-1H-isoquinolin compound, process for its preparation, and its use

Method of resolving stereoselectively racemic 2-alkyl-5-halopent-4-ene-carboxylic esters of the formula (I) 

The invention relates to R-hydroxynitrillyases from the family of Rosaceae that are characterized by an improved substrate tolerance and increased stability. In the active center of the R-hydroxynitrillyases either a) an alanine group is substituted by glycine, valine, leucine, isoleucine, or phenylalanine or b) a phenylalanine group is substituted by alanine, glycine valine, leucine or isoleucine, or c) a leucine group is substituted by alanine, glycine, valine, isoleucine or phenylalanine, or d) an isoleucine group is substituted by alanine, glycine, valine, leucine or phenylalanine. The invention also relates to the use of these lyases in the production of enantiomer-pure R- or S-cyanohydrines.

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New genes containing a DNA sequence coding for hydroxynitrile lyase, which genes can be prepared via a primer combination based on the DNA sequence of the 5'-region of the mdl genes from theand fromand/or a primer 2 based on the 3&#x2032;-region of the DNA sequences of one of the hydroxynitrile lyase isoenzymes fromor from, subsequent amplification with a DNA polymerase using a DNA from organisms, containing genes coding for hydroxynitrile lyase, as templates and cloning, and also recombinant proteins which can be prepared in suitable host cells by heterologous expression of the DNA sequence of said HNL genes, and proteins and fusion proteins derived therefrom and use of said proteins for preparing (R)- or (S)-cyanohydrins.

Isolated protein having hydroxynitrile lyase activity

A process for preparing enantiomer-enriched heterocyclic (R)- and (S)-cyanohydrins of the formula (I),  where R1, R2, R3, R4 independently of one another are H, an unsubstituted or substituted C&#x2013;C-alkyl, alkenyl or alkynyl radical, where one or more carbon atoms in the chain can be replaced by an oxygen atom, a nitrogen atom, a sulfur atom, an SO or an SOgroup, an unsubstituted or substituted aryl or heteroaryl radical or heterocyclic radical or halogen, hydroxyl, NR5R6, acetyl, oxo, C&#x2013;C-carbalkoxy, C&#x2013;C-carbalkoxyamino, COOR7, cyano, amide, benzoylamino or NO, R5 and R6 are H, C&#x2013;C-alkyl radical, phenyl radical, benzyl radical or COOR7, or together form a C&#x2013;C-alkylene or heteroalkylene radical, R7 is H or C&#x2013;C-alkyl, n is 0, 1, 2 or 3, X, Y and Z can be an unsubstituted or substituted carbon atom or a radical selected from the group consisting of N, O, S or NR5R6, where R5 and R6 are as defined above, SO or SO, and at least one of the radicals X, Y and Z is not a carbon atom, where the compounds of the formula (I) can have one or more double bonds in the ring, with the proviso that in a 5-membered ring the double bond is not conjugated with the &#x2014;C(OH)CN-group, and/or can be anellated and/or bridged, by reacting a ketone of the formula (II),  where R1, R2, R3, R4, X, Y, Z and n have the meanings above, with an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or two-phase system, or in emulsion, in the presence of a cyanide group donor.

Process for preparing heterocyclic (R)- and (S)-cyanohydrins

A process for preparing protected, enantiomer-enriched cyanohydrins of the formulawhere R1 and R2 independently of one another can be an unsubstituted, monosubstituted or polysubstituted C-C-alkyl, C-C-aryl, C-C-heteroaryl, C-C-alkaryl, C-C-alkylheteroaryl or C-C-aralkyl radical or an unsubstituted, monosubstituted or polysubstituted C-C-heterocycle, or C-C-alkylheterocycle or together can be an unsubstituted or substituted C-C-alkylene radical, which can contain one or more heteroatoms in the chain, or one of the radicals is hydrogen, and R3 can be an unsubstituted or substituted C-C-alkyl, C-C-aryl or C-C-heteroaryl radical, by reacting an aldehyde or ketone of the formulawhere R1 and R2 are defined as above, in the presence of an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or 2-phase system or in emulsion at a temperature of &#x2212;5 to +40&#xb0; C. with a carbonic ester nitrile of the formulawhere R3 is defined as above.

Process for preparing protected, enantiomer-enriched cyanohydrins by in-situ derivatization

New genes containing a DNA sequence coding for hydroxynitrile lyase, which genes can be prepared via a primer combination based on the DNA sequence of the 5'-region of the mdl genes fromand fromand/or a primer 2 based on the 3&#x2032;-region of the DNA sequences of one of the hydroxynitrile lyase isoenzymes fromor from, subsequent amplification with a DNA polymerase using a DNA from organisms, containing genes coding for hydroxynitrile lyase, as templates and cloning, and also recombinant proteins which can be prepared in suitable host cells by heterologous expression of the DNA sequence of said HNL genes, and proteins and fusion proteins derived therefrom and use of said proteins for preparing (R)- or (S)-cyanohydrins.

Genes containing a DNA sequence coding for hydroxynitrile lyase, recombinant proteins derived therefrom and having hydroxynitrile lyase activity, and use thereof

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Vienna, Austria

Wolfgang Skranc