摘要:
A process whereby 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, which are important intermediates of an HMG coenzyme A reductase atorvastatin, can be industrially, easily and efficiently produced. This process comprises starting with a 3,5-dihydroxy-6-halohexane derivative, treating it with a cyaniding agent to thereby substitute the halogen atom with the cyano group (i.e., a cyanation reaction) and forming an acetal of a diol by using an acetal-forming agent in the presence of an acid catalyst (i.e., an acetal-formation reaction).
摘要:
A nitrous acid salt is added at a temperature of 10 to 80°C to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).
摘要:
The present invention provides a method for safely producing a large amount of chloroformate compound with high yield. The chloroformate compound can be produced by mixing and reacting a solution of triphosgene ,an amine and an alcohol compound in a flow reactor. The chloroformate compound can also be produced by mixing and reacting a solution of triphosgene with a solution comprising an amine and an alcohol compound in a flow reactor. The amine is preferably tributylamine, and preferably used in an amount of 0.8 to 3 equivalents relative to an amount of the alcohol compound.
摘要:
The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.
摘要:
The present invention is related to a method of producing a peptide, characterized in contacting a reaction mixture with a base after a condensation reaction to hydrolyze while a basic condition is maintained until a ratio of a remaining unreacted active ester of an acid component is decreased to 1% or less in a liquid phase peptide synthesis method. According to the invention, a target peptide of high purity can be simply and efficiently produced by a continuous liquid phase synthesis method. Further, the present invention is related to a method of producing a peptide, characterized in using an amide-type solvent immiscible with water in a liquid phase peptide synthesis method. According to the invention, various peptides can be produced by the liquid phase synthesis method without being restricted by the amino acid sequence of the target peptide.
摘要:
The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxyalcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.
摘要:
A process whereby 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, which are important intermediates of an HMG coenzyme A reductase atorvastatin, can be industrially, easily and efficiently produced. This process comprises starting with a 3,5-dihydroxy-6-halohexane derivative, treating it with a cyaniding agent to thereby substitute the halogen atom with the cyano group (i.e., a cyanation reaction) and forming an acetal of a diol by using an acetal-forming agent in the presence of an acid catalyst (i.e., an acetal-formation reaction).
摘要:
A process by which an optically active epoxy alcohol derivative useful as an intermediate for medicines can be easily and industrially safely produced from an inexpensively available material; and a halohydrin derivative which is an important novel intermediate therefor. Also provided is a process for producing an intermediate for triazole type antifungal agents through a small number of steps, which comprises reacting the halohydrin derivative with a triazolesulfonamide. An optically active, substituted propionic ester derivative is reacted with a haloacetic acid derivative in the presence of a base to obtain an optically active haloketone derivative and this derivative is reacted with an arylmetal compound to stereoselectively obtain a halohydrin derivative. This halohydrin derivative is subjected to elimination of the substituent present on the hydroxy group and to epoxidation with a base to produce an optically active epoxy alcohol derivative.