Abstract:
The known nuclear hydroxylation of substituted phenols or phenol ethers with organic solutions of hydrogen peroxide in the presence of a catalyst is carried out in improved manner by employing both (1) a special, practically water free solution of hydrogen peroxide in an organic solvent which forms an azeotrope with water, which azeotrope boils below the boiling point of hydrogen peroxide, and (2) sulfur dioxide as a catalyst. Through this, the nuclear hydroxylation is substantially simpler than previously; difficult separations, e.g., from water-phenol, or the separation and recovery of the catalyst are eliminated. Besides, the yields are increased.
Abstract:
L-proline is produced from the methyl or ethyl ester of L-pyroglutamic acid by reacting this with at least twice the molar amount of phosgene to form the corresponding 1-chlorocarbonyl-5,5-dichloroproline ester, producing the corresponding 2-chloro-1-chlorocarbonyl-pyrrolin-(2)-carboxylic acid ester-(5) therefrom by splitting off hydrogen chloride, catalytically hydrogenating the pyrrolin-(2) compound to the corresponding N-chlorocarbonyl-proline ester and hydrolyzing the latter with acid to form L-proline.
Abstract:
The production of solutions of hydrogen peroxide in phenol or its derivatives, e.g. hydrocarbyl substituted phenols, halo substituted phenols or phenol ethers, is carried out in a single step. Practically no loss of hydrogen peroxide occurs since a total distillation of hydrogen peroxide together with phenol or phenol derivative is avoided. Simultaneously the solutions obtained are practically free from water. The mixture of phenol or phenol derivative and aqueous hydrogen peroxide is treated with a material that boils below the boiling point of hydrogen peroxide, phenol or phenol derivative or forms an azeotrope with water that boils below the boiling point of hydrogen peroxide, phenol or phenol derivative and the water removed as an azeotrope. The solution of hydrogen peroxide in phenol or phenol derivative which remains behind is suitable for carrying out oxidation reactions and above all, also for hydroxylation reactions.
Abstract:
The production of organic hydrogen peroxide solutions which are practically water-free until now has had the problem of either too high a water content of the solution or too great a loss of hydrogen peroxide through decomposition and passing over as distillate during the distillative drying. By selection of specific esters in combination with commensurately high pressures in the azeotropic removal of water, these disadvantages can be avoided. Extremely low water content solutions of hydrogen peroxide in high boiling solutions are produced by mixing hydrogen peroxide solutions in solvents whose azeotropic boiling point with water is below the boiling point of hydrogen peroxide with higher boiling solvents which form the highest azeotrope with water, whose boiling point is near or above the boiling point of hydrogen peroxide. Thereupon, the mixture is freed from both water and the lower boiling solvent. The mixture can be formed by an in situ method. Production of extremely low water containing solutions of hydrogen peroxide in high boiling solvents are produced by mixing hydrogen peroxide solutions in solvents whose azeotrope boiling point with water is below the boiling point of hydrogen peroxide with higher boiling solvents which form the highest azeotrope with water, whose boiling point is near or above the boiling point of hydrogen peroxide. Thereupon, the mixture is freed from both water and the lower boiling solvent. The above-mentioned mixture can also be produced by an in situ method.
Abstract:
The present invention relates to a screening process for hydantoin racemases and to novel hydantoin racemases, to the nucleic acid sequences coding therefor and to a proces for mutagenesis. Hydantoin racemases are of interest in connection with the production of enantiomerically enriched amino acids from racemic hydantoins.
Abstract:
A novel route is described for the synthesis of N-methyl-3-hydroxy-3-(2-thienyl)propylamine IV, which can be used as a starting compound for the preparation of duloxetine. N-methyl-3-hydroxy-3-(2-thienyl)propylamine is synthesized via novel thiophene derivatives containing carbamate groups, I and IIa, as intermediates.
Abstract:
A process is described for preparing optically active β-atninocarboxylic acids from racemic N-acylated β-aminocarboxylic acids by cnantiosclccthc hydrolysis of the N-acylated β-aminocarboxylic acid in the presence of a hydrolase by way of biocatalyst, wherein the N-acyl substituent of the N-acylated β-aminocarboxylic acid (I) exhibits Structure I in which R1, R2 are each selected, independently of one another, from H, halogen, alkiyl residues, OH, alkoxy residues and aryloxy residues; R3 is selected from halogen, alkoxy residues and aryloxy residues; (II) Structure IIA or IIB or the structure of the corresponding salts or (III) Structure III or the structure of the corresponding salt.
Abstract translation:描述了一种用于通过在水解酶存在下通过生物催化剂的N-酰化β-氨基羧酸水解N-外酰基化的β-氨基羧酸来制备光学活性β-阿魏酸的方法,其中N-酰基取代基 的N-酰化的β-氨基羧酸(I)表现出结构I,其中R 1,R 2各自彼此独立地选自H,卤素, 烷基残基,OH,烷氧基残基和芳氧基残基; R 3选自卤素,烷氧基残基和芳氧基残基; (II)结构IIA或IIB或相应盐的结构或(III)结构III或相应盐的结构。
Abstract:
A molecular weight-enlarged, homogeneously soluble ligand, useful in catalysts, particularly for the synthesis of enantiomerically enriched organic compounds, includes: a weight average molecular weight of at least 1000 g/mol; a molecular weight-enlarging polymer; optionally, a polymer linker; and at least one homochiral active center; wherein the active center is bound to the molecular weight-enlarging polymer through the polymer linker or is bound directly to the molecular weight-enlarging polymer.
Abstract:
Many inorganic substrates can be oxidized with a peroxo compound, such as hydrogen peroxide. In processes which are already known, pure alkylrhenium oxides of the formula RaRebOcLd are employed. Catalyst compositions such as are obtainable from the reaction of an oxorhenium compound of the formula ReOmAn with an organylating agent, in particular a Grignard compound, without the preparation process comprising an expensive sublimation, crystallization or distillation, can be employed with the same activity in the oxidation reactions. In addition to oxidation processes, catalyst compositions are disclosed.
Abstract:
The present invention relates to the preparation of compounds of formula (I): from the corresponding hydantoins by means of an enzymatic process. The L-compound is preferably formed.