Abstract: The present invention relates to a novel biocatalytic process for the stereoselective preparation of alpha amino amide compounds catalyzed by NHase enzymes. A further aspect of the invention relates to novel NHase enzymes as well as further improved NHase enzyme mutants, nucleic acid molecules encoding these enzymes, recombinant microorganisms suitable for preparing such enzymes and mutants. Another aspect of the invention relates to a chemo-biocatalytic process for the preparation of lactam compounds comprising the new catalytic process for the preparation of alpha amino amide compounds catalyzed by NHase enzymes, as well as the chemical oxidation of the alpha amino amide by applying certain chemical oxidation catalysts suitable for converting the alpha amino amide under retention of its stereochemical configuration to the respective lactam. The novel chemo-biocatalytic process is particularly suited for the synthesis of valuable pharmaceutical compounds, like in particular (S)-Levetiracetam.

Abstract: The present invention relates to regioselective chemical and electrochemical processes for the preparation of an oxidized heterocyclic alpha-amino amide compounds. By applying specific catalysts or catalyst systems during chemical oxidation or by applying particular electrochemical oxidation conditions the present invention provides access to valuable alpha amino amide compounds, which are oxidized at the heterocyclic amino group by regioselective introduction of either a hydroxyl or a keto group. In a more particular embodiment, the present invention describes a chemical oxidation reaction, which advantageously is applicable in the enantioselective synthesis of valuable oxidized heterocyclic alpha-amino amide compounds, like levetiracetam, brivaracetam or the synthesis of piracetam. Another aspect of the present invention relates to a process for the electrochemical recycling of alkali perhalogenate oxidants as spent during said regioselective oxidation reactions of the invention.

Abstract: In various aspects and embodiments the invention provides a method for preparing a metal periodate by anodic oxidation of a metal iodide in an electrolysis cell comprising one or more anodes and one or more cathodes, characterised in that the one or more anodes are carbon-comprising electrodes. In certain embodiments the method is characterised in that the one or more anodes comprise a diamond layer doped with one or more IUPAC group 13, 15 or 16 elements of the periodic table.

Abstract: The present invention relates to an improved process for preparation of Ozanimod (I) or pharmaceutically acceptable salts thereof. The present invention also relates to an improved process for preparation of (S)-1-amino-2,3-dihydro-1H-indene-4-carbonitrile (II) or its optically active acid salts.

Abstract: The present invention is directed to a process for the enantioselective biocatalytic preparation of 4-substituted 1-aminoindanes of general formula (S)-I: (1) and a process for the preparation of Ozanimod, preferably involving the enantioselective biocatalytic process of preparing (S)-4-substituted 1-aminoindanes of the above general formula, wherein R=—CN and Y=H.

Abstract: A process of diminishing the concentration of a transition metal complex from a first solution by adding a solubility-enhancing compound that enhances the solubility of said complex in a second solution and extracting the first solution with the second solution. The solubility-enhancing compound is a compound of formula A wherein, Ra is SH, SO3H, OH or COOH; Rb is SH, OH or COOH; Rc each independently is H, SH, OH or COOH; Rd each independently is H or COOH; n is 1, 2, 3, 4 or 5; or a salt or an activated form thereof.

Abstract: An improved process for making 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-di pyrido[3,2-b:2?,3?-e][1,4]diazepin-6-one.

Abstract: Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

Abstract: The invention relates to a crystalline sodium salt of 4?-[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.

Abstract: A process of diminishing the concentration of a transition metal complex from a first solution by adding a solubility-enhancing compound that enhances the solubility of said complex in a second solution and extracting the first solution with the second solution. The solubility-enhancing compound is a compound of formula A wherein, Ra is SH, SO3H, OH or COOH; Rb is SH, OH or COOH; Rc each independently is H, SH, OH or COOH; Rd each independently is H or COOH; n is 1, 2, 3, 4 or 5; or a salt or an activated form thereof.

Abstract: Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

Abstract: The invention relates to a crystalline sodium salt of 4′-[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.

Abstract: The invention relates to a crystalline sodium salt of 4′-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.

Abstract: The invention relates to a crystalline sodium salt of 4′-[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.