Abstract: The present invention provides a crystalline 2,4-bridged common intermediate useful for producing a plurality of ENA monomers, a method for stereoselectively producing the intermediate, and a method for efficiently producing ENA monomers using the intermediate.

Abstract: Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use. Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit possesses excellent solubility and a safety profile for use in humans for the treatment of bacterial infectious diseases.

Abstract: Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use. Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit possesses excellent solubility and a safety profile for use in humans for the treatment of bacterial infectious diseases.

Abstract: A method of manufacturing a compound represented by the formula R1C(OR7)3, wherein R1 represents a C1-C19 alkyl group and R7 represents a C1-C6 alkyl group by reacting a compound represented by the following formula (15): wherein R1 represents a C1-C19 alkyl group, R7 represents a C1-C6 alkyl group and X represents Cl, Br, I, HSO4 or NO3, with a compound represented by the formula R7—OH, wherein R7 represents a C1-C6 alkyl group, in a solvent which forms a bilayer system.

Abstract: A method for manufacturing a compound represented by the following formula (I): wherein R1 represents a C1-C19 alkyl, R2 represents a C1-C4 alkyl, and Ac represents an acetyl, wherein the compound of the formula (I) is optionally contained with up to 10 wt. % of a compound represented by the following formula (II): or a pharmacologically acceptable salt thereof, involving reacting a compound represented by the following formula (13): wherein R2 represents a C1-C4 alkyl and Ac represents an acetyl, with a compound represented by the formula R1C(OR7)3, wherein R1 represents a C1-C19 alkyl and R7 represents a C1-C6 alkyl, or a pharmacologically acceptable salt thereof.

Abstract: A compound represented by the following formula (I): wherein R1 represents a C1-C19 alkyl, R2 represents a C1-C4 alkyl and Ac represents an acetyl, the compound represented by the formula (I) is optionally contained with up to 10 wt. % of a compound represented by the following formula (II): having a chemical purity of 97 wt. % or higher, wherein in the case where the compound represented by the formula (II) is contained with the compound represented by formula (I), the chemical purity of the mixture of the compound represented by the formula (I) and the compound represented by the formula (II) is 97 wt. % or higher.

Abstract: A method of manufacturing a compound represented by the formula R1C(OR7)3, wherein R1 represents a C1-C19 alkyl group and R7 represents a C1-C6 alkyl group by reacting a compound represented by the following formula (15): wherein R1 represents a C1-C19 alkyl group, R7 represents a C1-C6 alkyl group and X represents Cl, Br, I, HSO4 or NO3, with a compound represented by the formula R7—OH, wherein R7 represents a C1-C6 alkyl group, in a solvent which forms a bilayer system.

Abstract: An object of the present invention is to provide a pyrrole derivative useful as an immunosuppressive agent and a method for producing the same. For achieving the object, the present invention provides a method for producing a compound represented by the general formula (I) by heating a compound represented by the general formula (III) and a compound represented by the general formula (IV) in a nonpolar solvent under reduced pressure.

Abstract: An object of the present invention is to provide a pyrrole derivative useful as an immunosuppressive agent and a method for producing the same. For achieving the object, the present invention provides a method for producing a compound represented by the general formula (I) by heating a compound represented by the general formula (III) and a compound represented by the general formula (IV) in a nonpolar solvent under reduced pressure.

Abstract: A method for manufacturing a compound represented by the formula (13): wherein R2 represents a C1-C4 alkyl group and Ac represents an acetyl group, including reacting a compound represented by the following formula (12): wherein R2 represents a C1-C4 alkyl group, Ac represents an acetyl group and Boc represents a tert-butoxycarbonyl group, with water.

Abstract: A method for manufacturing neuraminic acid derivatives is provided, also synthetic intermediates of the neuraminic acid derivatives and methods for their manufacture, and neuraminic acid derivatives having high purity. [Means for Solution] A synthetic intermediate compound represented by the formula (7) is provided: [wherein R3 represents alkyl; R4 and R5 each represents H, alkyl, phenyl, or together represent tetramethylene, pentamethylene, oxo].

Abstract: A method for manufacturing neuraminic acid derivatives is provided, also synthetic intermediates of the neuraminic acid derivatives and methods for their manufacture, and neuraminic acid derivatives having high purity. [Means for Solution] A synthetic intermediate compound represented by the formula (7) is provided: [wherein R3 represents alkyl; R4 and R5 each represents H, alkyl, phenyl, or together represent tetramethylene, pentamethylene, oxo].

Abstract: An optically active 4,4-di-substituted oxazolidine compound having the formula (I) wherein R1 represents a substituted C1-C3 alkyl group, a substituted C2-C3 alkenyl group, a formyl group, a hydroxymethyl group, a group of the formula COOR, a halogenated methyl group, a phosphonium methyl group; R represents a C1-C6 alkyl group, a C2-C6 alkenyl group, a phenyl group or a benzyl group; R2 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, or a phenyl group; R3 represents a C2-C6 alkanoyl group, a C1-C6 alkyloxycarbonyl group, a benzoyl group, a phenyloxycarbonyl group or a benzyloxycarbonyl group and R4 represents a C1-C6 alkyl group or a C2-C6 alkenyl group.

Abstract: An optically active 4,4-di-substituted oxazolidine compound having the formula (I) wherein R1 represents a substituted C1-C3 alkyl group, a substituted C2-C3 alkenyl group, a formyl group, a hydroxymethyl group, a group of the formula COOR, a halogenated methyl group, a phosphonium methyl group; R represents a C1-C6 alkyl group, a C2-C6 alkenyl group, a phenyl group or a benzyl group; R2 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, or the like or a phenyl group; R3 represents a C2-C6 alkanoyl group, a C1-C6 alkyloxycarbonyl group, a benzoyl group, a phenyloxycarbonyl group or a benzyloxycarbonyl group and R4 represents a C1-C6 alkyl group or a C2-C6 alkenyl group.

Abstract: Hydrates of the compound of formula (I) and crystalline forms thereof have excellent storage stability and are useful medicaments.

Abstract: Hydrates of the compound of formula (I) and crystalline forms thereof have excellent storage stability and are useful medicaments.