Clariant Corporation

Archimica Gmbh

Euticals Gmbh

Andreas Meudt

Stefan Scherer

Steffen Haber

Frank Vollmueller

Claudius Boehm

Antje Noerenberg

Michael Erbes

Frank Vollm&uuml;ller

Richard Wisdom

Holger Geissler

Joerg Jung

Klaus Forstinger

Alexei Kalinin

Victor Snieckus

Wilfried Pressler

Robert Cosmo

Heinz Georg Kautz

Quofang Qiu

Paul Meek

Peter Koch

Sven Nerdinger

Gerhard Demmer

Bernd Lehnemann

Jason Helmke

Jörg Jung

Till Vogel

Claudius Böhm

The invention relates to a process for the asymmetric transfer hydrogenation of a ketone substrate to produce as chiral secondary alcohol with an ee of greater than 85% in which an enantio-enriched chiral catalyst containing ruthenium or rhodium is used with a hydrogen donor and in which an anion exchange resin is used as a base.

Process for the asymmetric transfer hydrogenation of ketones

The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20&#xb0; C. 

Process for producing lacosamide

The invention relates to processes for preparing acylated amphetamine, methamphetamine and dexamphetamine derivatives by reacting the parent amine with the to be-coupled acid or a salt of the to-be coupled acid which acid is optionally protected, in the presence of an alkylphosphonic acid anhydride as coupling agent and, if the acid was protected then cleaving the protecting group(s), in a one-pot reaction or in two or more separate steps.

Process for the synthesis of amphetamine derivatives

Process for preparing nitriles by reacting N-alkylcarboxamides (RCO&#x2014;NHR) or ammonium salts of carboxylic acids (RCOO&#x2014;NHR) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NHR, RCOOH+NHR), respectively, R being an arbitrarily substituted linear or branched C-C-alkyl radical, a C-Ccycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and Rbeing an arbitrary substituted, linear or branched C-Calkyl radical, a C-Ccycloalkyl radical or an alkenyl or alkynyl radical, with phosphonic anhydrides in the presence of an optional base in an organic solvent at a temperature in the range from &#x2212;30 to 180&#xb0; C. In advantageous embodiments, the phosphonic anhydride is a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane 2,4,6-trioxide of the formula (I) 

Process for preparing nitriles by elimination reactions

A method for producing unprotected or carbamate-protected amines of formulae (II) and (III) or R&#x2014;NH(II) or R&#x2014;NHCOR(III) by reacting hydroxamic acids of formula (I) (RCONHOH) with a) alkylpliosphonic acid anhydrite's, b) alcohol ROH and c) optionally with a base, at a temperature ranging from 100 to +120&#xb0;C., wherein the hydroxainic acid (I) is produced prior to or during reacting (in situ) and Ris an optionally substituted linear or branched C-Calkyl radical, substituted C-Ccycloalkyl, alkenyl, aryl or heteroaryl radical and Ris an open-chain, cyclic or branched allyl, aryl or Cto C-alkyl radicals, or aryloxy, allyloxy or alkoxy radical possibly substituted with open-chain, cyclic or branched Cto C-alkyl radicals.

Method for producing amines from hydroxamic acids

The invention relates to a method for producing the nitrites of formula: R&#x2014;CN by reacting aldehyde oximes (RCN&#x2550;N&#x2014;OH) with cyclic alkylphosphonic anhydrides at a temperature ranging from &#x2212;100 to +120&#xb0; C., wherein Rrepresents H, a linear or branched C-Calkyl group, a C-Ccycloalkyl, alkenyl or an aryl or heteroaryl group. The cyclic phosphonic anhydride preferably used is a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide of formula (I), wherein R' independently represents allyl, aryl or open-chain or branched Cto Calkyl groups. Optionally, the reaction can be carried out in the presence of a tertiary amine base NR 

Method for producing nitriles by elimination of water from aldehyde oximes with alkylphosphonic anhydrides

The invention relates to a method for the production of a.) aldehydes of formula (II): R&#x2014;CHO and b.) aldehydes of formula (III): R&#x2014;C(O)&#x2014;Rby reacting a.) primary alcohols (RCH&#x2014;OH) or b.) secondary alcohols (R&#x2014;CH(OH)&#x2014;R) with cyclic phosphonic acid anhydrides in the presence of dialkyl-, diaryl- and/or alkyl-aryl sulphonic oxides at a temperature in the region of between &#x2212;100 to +120&#xb0; C., whereby Rand/or Rrepresent H, a substituted linear or branched C-C-alkyl radical, a substituted C-Ccycloalkyl-, alkenyl-, aryl- or heteroaryl radical. A cyclic phosphonic acid anhydride is used, preferably, as a 2,4,6-substituted 1,3,5,2,4,6-trioxatriphosphinane of formula (I), wherein R' independently represents allyl, aryl or open-chained or branched C-C-alkyl-radicals. Optionally, the reaction can be carried out in the presence of a tertiary amine base NR 

Method for the production of aldehydes and ketones by oxidizing primary and secondary alcohols with alkylphosphonic acid anhydrides

A method for preparing aryllithium compounds of the formulae (IV) and (VI) includes reacting halogen compounds (I) with lithium metal to obtain a lithium compound of formula (II) and reacting the lithium compound of formula (II) with aromatic compounds of the formulae (III) and/or (V) to form lithium aromatics (IV) and (VI).

Method for producing, via organometallic compounds, organic intermediate products

A process for preparing anilineboronic acid derivative of the formula I, by converting an aniline to a diprotected aniline by introducing two protecting groups, metalating the diprotected aniline with a metalating agent and simultaneously or subsequently reacting with a boronic ester B(OR)to form a protected anilineboronic ester, which is converted, by detaching the protecting groups, to the anilineboronic esters of the formula (I).

Preparation of Anilineboronic acids and derivatives thereof

A process for preparing compounds of the formula (II),where the substituents Rto Rare each independently H, CH, straight-chain or branched C&#x2013;C-alkyl, CH(OC&#x2013;C-alkyl), CH(C&#x2013;C-alkyl)(OC&#x2013;C-alkyl), CH(OC&#x2013;C-alkyl), CH(CH)(OC&#x2013;C-alkyl), C&#x2013;C-alkoxy, N(C&#x2013;C-alkyl), phenyl, substituted phenyl, aryl, heteroaryl, S(C&#x2013;C-alkyl) or a radical C, andthe symbols Xare each carbon or a maximum of two neighboring Xare nitrogen or XRand XRtogether are O, NH, N(C&#x2013;C-alkyl), N(C&#x2550;O&#x2014;C&#x2013;C-alkyl), N(SiR)or S,or where neighboring radicals Rto Rform the following structural unit,where Xto Xand Rto Rhave the same meaning as Xto Xand Rto Rwhich comprises reacting chloro- or fluoroaromatics of the formula (I) with carbon electrophiles and lithium metal.

Preparation of substituted aromatic compounds

Method for producing formylphenylboronic acids

Process for the preparation of substituted phenylboronic acids

A process for preparing 4-substituted 2-alkylbiphenyls and 2-alkoxybiphenyls of the formula (I),

Process for preparing 4-substituted 2-alkylbiphenyls and 2-alkoxylbiphenyls

Process for preparing highly pure formylphenylboronic acids

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Flörsheim-Weilbach, Germany

Andreas Meudt