Abstract: A process for the preparation of an enantiomerically enriched amine, is performed by a) cleaving a racemic mixture of a reaction product of i) a chiral amine and ii) an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; or b) reacting an amine with an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; and c) separating the enantiomerically enriched amide from the enantiomerically enriched amine, wherein the acyl donor is a sulphonylacetic acid ester. The process (1) leads to high enantioselectivities, and (2) high reactivities, (3) is based on an acyl donor accessible in a simple manner, (4) is suitable for a large number of very different substrates and/or (5) is suitable for carrying out at high substrate concentrations.

Abstract: (Hetero)aromatic are prepared from halogen-substituted (hetero)aromatic compounds in the presence of a base and a palladium catalyst having a nonpyrophoric monodentate phosphane ligand. The phosphane ligand structure includes two radical groups having a tertiary carbon attached directly to phosphorous and one radical group having a primary carbon attached to the phosphorous.

Abstract: The present invention relates to a process for the preparation of compounds of the general formula (I). These are used as important intermediates in the preparation of bioactive substances. Preparation is carried out starting from dicarbonyl compounds of the general formula (II), which are reacted with appropriate hydrazine derivatives of the general formula (III) and subsequently hydrogenated. The present invention also relates to advantageous intermediate compounds.

Abstract: The present invention is aimed at a process for the preparation of enantiomerically enriched compounds of general formula (I). These are obtained by classical resolution of the corresponding acid using a chiral amino base in organic solvents.

Abstract: The present invention is aimed at a process for the preparation of (hetero)aromatic aldehydes. The aldehydes are obtained from corresponding Hal?-substituted (hetero)aromatics by palladium-catalysed reductive carbonylation in the presence of a specific monodentate phosphane-based ligand system.

Abstract: The present invention is aimed at a process for the preparation of enantiomerically enriched compounds of general formula (I). These are obtained by classical resolution of the corresponding acid using a chiral amino base in organic solvents.

Abstract: A process for the preparation of an enantiomerically enriched amine, is performed by a) cleaving a racemic mixture of a reaction product of i) a chiral amine and ii) an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; or b) reacting an amine with an acyl donor, in the presence of a hydrolase, to obtain a mixture of an enantiomerically enriched amide and an enantiomerically enriched amine; and c) separating the enantiomerically enriched amide from the enantiomerically enriched amine, wherein the acyl donor is a sulphonylacetic acid ester. The process (1) leads to high enantioselectivities, and (2) high reactivities, (3) is based on an acyl donor accessible in a simple manner, (4) is suitable for a large number of very different substrates and/or (5) is suitable for carrying out at high substrate concentrations.

Abstract: The present invention is concerned with a process for preparing compounds of the general formula (I). These compounds can preferably be used to prepare bioactive agents. The reaction of the invention starts from the corresponding hydroxy compounds which are oxidized, with Ru catalysis, in a one-phase aqueous system.

Abstract: 5-formyl-2-furylboronic acid is produced by a) adding a base to a composition containing a boric acid ester and 2-furaldehyde, thereby obtaining a reaction mixture and protecting the formyl group of said 2-furaldehyde with a protective group, b) working-up of the reaction mixture in an acidic medium, and c) isolating of the 5-formyl-2-furylboronic acid.

Abstract: The present invention relates to a process for the preparation of compounds of the general formula (I) by catalytic enantioselective hydrogenation of the corresponding ketones. There are used inter alia ruthenium catalysts with chiral diamines and chiral biphosphines as ligands.

Abstract: 5-formyl-2-furylboronic acid is produced by a) adding a base to a composition containing a boric acid ester and 2-furaldehyde, thereby obtaining a reaction mixture and protecting the formyl group of said 2-furaldehyde with a protective group, b) working-up of the reaction mixture in an acidic medium, and c) isolating of the 5-formyl-2-furylboronic acid.

Abstract: The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

Abstract: The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

Abstract: The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Abstract: The present invention is directed towards a process for the preparation of enantiomerically enriched 4-hydroxymethyl-&ggr;-butyrolactone (I). By kinetic racemate cleavage of racemic epoxide of the general formula (II) wherein R represents a (C1-C8)-alkyl radical, a (C8-C16)-aryl radical, with a nucleophile and a Jacobsen catalyst there is obtained enantiomerically enriched (I). Use of the lactone so prepared.

Abstract: The invention relates to an enzymatic method for reductive amination of &agr;-ketodicarboxylic acid derivatives or salts thereof using an amino acid dehydrogenase.

Abstract: The present invention is concerned with novel processes for the preparation of (2R-cis)-2-[[1-[3.5-bis(trifluoromethyl)phenyl]ethenyl]oxy]-3-(4-fluorophenyl)-4-(phenylmethyl) mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Abstract: A process of synthesizing a compound of structural formula 6 is disclosed wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents a benzyl, C1-6 alkyl or aryl; Y represents C1-3 alkyl, O, NH or S; X represents O, NH, or S and R5 represents a carboxy protecting group, comprising reacting a compound of formula 5: wherein R1, R2, R5, X and Y are as previously described with a phosphite or phosphonite reagent to produce a compound of formula 6. Further disclosed is an efficient method for the synthesis of a compound of formula 2: which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.

Abstract: N-methyleneglycinates of formula (I) 1

Abstract: The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.