Abstract: The invention relates to acid addition salts of ridinilazole and processes for the preparation of ridinilazole using these acid addition salts. In addition, the present invention relates to processes for the preparation of ridinilazole in pure form using acid addition salts of ridinilazole as process intermediates.

Abstract: The invention relates to acid addition salts of ridinilazole and processes for the preparation of ridinilazole using these acid addition salts. In addition, the present invention relates to processes for the preparation of ridinilazole in pure form using acid addition salts of ridinilazole as process intermediates.

Abstract: The present invention relates to processes, process steps and intermediates useful in the asymmetric bisamidation of malonic ester derivatives wherein the new processes, process steps and intermediates are, for example, useful in the preparation of asymmetric malonic acid bisanilides such as cabozantinib.

Abstract: A process for the preparation of a compound of formula (I) and of a acid salt (T) wherein R1 is selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R2 and R3, are, independently of each other, selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R4, R5, R6 and R7, are independently of each other, selected from the group consisting of H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, and wherein the acid salt is a 2,3-Ditoluoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid salt, 2,3-Dianisoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid mono(dimethylamide) salt or a mixture of two or more thereof, wherein the tartaric acid salt (T) of the compound of formula (I) contains at least 90% by weight of the tartaric salt of the compound of formula (Ia) based on the total weight of the acid salt of the compound of formula (I).

Abstract: Process for preparing nitriles by reacting N-alkylcarboxamides (RCO—NHR1) or ammonium salts of carboxylic acids (RCOO—NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NH2R1, RCOOH+NH3R1+), respectively, R being an arbitrarily substituted linear or branched C1-C12-alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl 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 ?30 to 180° C.

Abstract: A process for the manufacture of aminocarbonyl boronic acids of formula (IV) by converting the compounds of formula (III) with a Brønsted base Y(OH)n in a solvent or a solvent mixture, in which Z represents an optionally substituted arylene, heteroarylene, alkene, heteroalkene, alkylidene, heteroalkylidene, alkenylidene, heteroalkenylidene, alkynylidene, arylalkylene, heteroarylalkylene, arylheteroalkylene, heteroarylheteroalkylene, alkylheteroarylene, heteroalkylheteroarylene, or alkylarylene group; Y represents a metal or ammonium cation of valence n with 0<n<5; and B represents boronic acid, boronic acid ester, or a borate, or a boronic acid anhydride. The aminocarbonyl boronic acids of formula (IV) can be further hydrolyzed to form the carboxy boronic acid of formula (V).

Abstract: The invention relates to a method for producing alkyl-substituted aromatic and heteroaromatic compounds by cross-coupling alkyl boronic acids with aryl- or heteroaryl-halogenides or with aryl- or heteroaryl-sulfonates in the presence of a catalyst and of a Brönsted base in a solvent or solvent mixture.

Abstract: The invention relates to a method for producing aryl or heteroaryl amines, ethers or thioethers (III) by cross-coupling primary or secondary amities, alcohols or thioalcohols with substituted aryl or heteroaryl compounds (I) in the presence of a Brønsted base and a catalyst or a pre-catalyst containing a) a transition metal, a complex, a salt, or a compound of a transition metal from the group V, Mn, Fe, Co, Ni, Rh, Pd, Ir, Pt, and b) at least one sulfonated phosphane ligand in a solvent or a solvent mixture corresponding to Scheme 1 wherein Hal represents fluorine, chlorine, bromine, iodine, alkoxy, trifluoromethane sulfonate, nonafluorotrimethyl-methane sulfonate, methane sulfonate, 4-nitrobenzene sulfonate, benzene sulfonate, 2-naphthalene sulfonate, 3-nitrobenzene sulfonate, 4-nitrobenzene sulfonate, 4-chlorobenzene sulfonate, 2,4,6-triisopropylbenzene sulfonate or any other sulfonate, and X represents O, S or NR?. The invention also relates to novel phosphane ligands.

Abstract: Process for preparing nitriles by reacting N-alkylcarboxamides (RCO—NHR1) or ammonium salts of carboxylic acids (RCOO—NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH+NH2R1, RCOOH+NH13R1+) respectively, R being an arbitrarily substituted linear or branched C1-C12-alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl 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 ?30 to 180° C.

Abstract: Process for preparing compounds by cross-coupling of enolizable carbonyl compounds, nitriles or their analogues with substituted aryl or heteroaryl compounds in the presence of a Brönsted base and of a catalyst or precatalyst containing a.) a transition metal, a complex, a salt or a compound of this transition metal from the group V, Mn, Fe, Co, Ni, Rh, Pd, Ir, Pt) and b.) at least one sulphonated phosphane ligand in a solvent or solvent mixture.

Abstract: Methods for producing furfural-4-boronic acid by the reaction of furfural acetals (I), which are substituted by halogen in position 4, with boronic acid esters or anhydrides, by the subsequent metalation of compound (I) and the simultaneous or subsequent reaction with a boronic acid ester or anhydride to form an acetal-protected furfural-4-boronic acid ester. This product is subjected to acid hydrolysis to form furfural-4-boronic acid. In the formulae: X represents chlorine, bromine or iodine; R represents a branched, unbranched and/or cyclic, optionally substituted C1-C20 alkyl group, an optionally substituted C6-C12 aryl group or an optionally substituted C3-C8 cycloalkyl group, the two groups R together can form a ring; R?, R?, R?? independently of one another represent acylic or cyclic, branched or unbranched, optionally substituted C1-C20 alkyl groups, or optionally substituted aryl groups, optionally two of the groups R?, R? and R?? together form a ring, or represent additional groups B(OR)3.

Abstract: The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of Factor Xa and for the treatment and/or prevention of diseases that are mediated by Factor Xa activity.

Abstract: The invention concerns a method for producing: a) nitriles of formula (II) and b) isonitriles of formula (III) by reacting: a) carboxylic acid amides (RCO—NH2), ammonium salts of carboxylic acids (RCOO—NH4+) or carboxylic acids in the presence of ammonia or ammonium salts (RCOOH+NH3, RCOOH+NH4+) or b) formamides (H—CO—NHR) or mixtures of amines with formic acid, with cyclic phosphonic acid anhydrides while eliminating water at a temperature ranging from ?30 to +120° C., in which R represents an arbitrarily substituted linear or branched C1-C8 alkyl radical, a C3-C10 cycloalkyl radical, alkenyl radical, alkynyl radical or an aryl radical or heteroaryl radical.

Abstract: The present invention relates to the use of a compound of formula (I): 1