Abstract:
It is intended to provide a process for conveniently producing on an industrial scale an optically active .alpha.-methylcysteine derivative or it s salt in the form of an L- or D-compound, which is useful as an intermediate of a drug, etc., from a less expensive and easily available material. Namely, a process for producing an optically active .alpha.-methylcysteine derivative or its salt in the form of an L- or D-compound which comprises D-selectively cyclizing a racemic N-carbamoyl-.alpha.-methylcysteine derivative or its sal t with the use of hydantoinase to give a D-5-methyl-5-thiomethylhydantoin derivative or its salt and N-carbamoyl-.alpha.-methyl-L-cysteine derivative or its salt, and then deblocking and hydrolyzing the amino group and the sulfur atom of each product.
Abstract:
The present invention is to efficiently and simply prepare an optically active 7-substituted-2-aminotetralin with industrial advantage. In the process, a 7-substituted-2-tetralone or its bisulfite adduct is reduced with a microorganism to an optically active 7-substituted-2-tetralol. Then, a sulfonyl group is introduced to the hydroxy group to form an optically active 7-substituted-2-sulfonyloxytetralin. Then, with inversion of the configuration, a nitrogen substituent is introduced using a nitrogen nucleophile to form an optically active 2,7-substituted tetralin. Furthermore, if necessary, the nitrogen substituent is converted into a non-substituted amino group. Thus, an optically active 7-substituted-2-aminotetralin or its salt is prepared.
Abstract:
A process for producing porous cellulose beads of the present invention is characterized by comprising the steps of: a) mixing an alkali aqueous solution and cellulose to prepare cellulose micro dispersion at low temperature, b) adding water to the cellulose micro dispersion to prepare cellulose slurry, and d) bringing the cellulose slurry into contact with coagulation solvent. A carrier for ligand immobilization of the present invention is characterized by being by shrinking polysaccharide porous beads not less than 10% by a shrinkage rate defined by the following formula, and crosslinking the polysaccharide porous beads: Shrinkage rate % = 1 ˆ’ V 2 / V 1 × 100 (wherein, V 1 indicates the gel volume of polysaccharide porous beads before shrinkage, and V 2 indicates the gel volume of polysaccharide porous beads after shrinkage).
Abstract:
An industrially advantageous process for preparing high-purity 3-hydroxytetrahydrofuran easily and simply, which comprises converting a 4-halo-3-hydroxybutyric acid ester into a 4-halo-1,3-butanediol by reducing the ester with a boron hydride compound and/or an aluminum hydride compound in an organic solvent incompatible with water and treating the obtained reaction mixture with an acid and water, recovering an aqueous solution containing the diol, conducting the cyclization of the diol in this aqueous solution, extracting the resulting solution with an organic solvent incompatible with water, and isolating 3-hydroxytetrahydrofuran from the extract through concentration and/or distillation.
Abstract:
A process for preparing optically active azetidine -2-carboxylic acid efficiently, easily, simply, and industrially advantageously by cyclizing an optically active 4-amino- 2-halogenobutyric acid in an optical yield of as high as 90 % or above. Specifically, a process for preparing optically active azetidine-2-carboxylic acid of formula (2) (wherein * represents an asymmetric carbon atom) by cyclizing an optically active 4-amino-2-halogenobutyric acid of the general formula (1) (wherein X is halogeno and * represents an asymmetric carbon atom) in the presence of an alkaline earth metal oxide, an alkaline earth metal hydroxide except barium hydroxide, or an organic amine.
Abstract:
The application is concerned with a process for producing a 3-hydroxytetrahydrofuran of the formula (3): by cyclizing a 4-halo-1,3-butanediol of the general formula (2): wherein X represents a halogen atom in an aqueous solution, which comprises carrying out the cyclization reaction under weakly acidic to neutral conditions. Furthermore several methods are disclosed for the isolution of highly pure 3-hydroxytetrahydrofuran.
Abstract:
A process for easily producing an L- alpha -methylcysteine derivative or its salt, which is useful as a drug intermediate, from a cheap easily procurable raw material through an enzymatic D-stereoselective hydrolysis of racemic 5-halomethyl-5-methyl-hydantoin. L- alpha -methylcysteine derivative or its salt is produced by converting racemic 5-halomethyl-5-methylhydantoin to L-5-halomethyl-5-methylhydantoin through an enzymatic D-stereoselective hydrolysis, reacting the L-5-halomethyl-5-methylhydantoin with a sulfurizing agent into L-5-methyl-5-thiomethylhydantoin and hydrolyzing the L-5-methyl-5-thiomethylhydantoin.