Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing a carbamate compound, which is simple and industrially suitable.SOLUTION: The method includes reacting an amine compound and a carbonate compound in the presence of a hydrolytic enzyme catalyst and in the absence of a solvent. According to this, an intended carbamate compound can be industrially suitably produced in good yield.
Abstract:
PROBLEM TO BE SOLVED: To provide a method for industrial production of an (R or S)-N-substituted-β-amino acid and its ester having a reverse absolute steric configuration while suppressing autohydrolysis of a β-amino acid ester liable to be hydrolyzed with water, and improving yield, selectivity, operability, etc., of an optically active N-substituted-β-amino acid difficult to obtain in an isolated state.SOLUTION: An optically active (R or S)-N-substituted-β-amino acid is formed and an unreacted optically active (S or R)-N-substituted-β-amino acid alkyl ester is obtained by selectively reacting one enantiomer of an N-substituted-β-amino acid alkyl ester (racemic mixture) expressed by general formula (I) (in the formula, P is a protecting group; Ris alkyl, alkenyl, cycloalkyl, aralkyl or aryl; and R is alkyl) with water in an organic solvent in the presence of a hydrolase.
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing a polycarbonate diol diacrylate compound from polycarbonate diol and an acrylic ester compound without using a protonic acid and a metal component.SOLUTION: In the method for producing a polycarbonate diol diacrylate compound, polycarbonate diol represented by formula (I) is reacted with an acrylic ester compound represented by formula (II) in the presence of lipase. In formula (I), each Ris the same or different and a divalent group composed of one or more straight chain, branched chain, or cyclic alkylene groups, wherein the divalent group may have a substituent and/or one or more non-terminal carbon atoms substituted with a divalent aromatic group, a divalent heterocyclic group, an oxygen atom, or a sulfur atom, or is a divalent group of a crosslinking carbocyclic ring; and n represents an average degree of polymerization and is a number of 1-50. In formula (II), Ris a hydrogen atom or a 1-4C straight chain or branched chain alkyl group; and Ris a 1-12C straight chain, branched chain or cyclic alkyl group, a 7-10C aralkyl group or a 6-10C aryl group.
Abstract:
PROBLEM TO BE SOLVED: To obtain the subject compound capable of readily industrializing and useful as an antiallergic agent having antileukotriene action without using a solvent affecting adverse influence on environment by using an ester-based solvent or amide-based solvent as an organic solvent. SOLUTION: When (A) a quinaldine derivative (e.g. quinaldine) of formula I (R to R are each H or a halogen) is reacted with (C) a brominating agent (e.g. N-bromosuccinimide) in the presence of (B) a free radical initiator (e.g. N,N'-azobisisobutyronitrile), the reaction is carried out in a solvent expressed by the formula R COR [R is H, an alkyl or an alkoxy; R is an alkoxy or NR 2 (R is an alkyl)], preferably an ester-based solvent or an amide-based solvent, especially ethyl acetate or dimethylformamide to provide the objective compound of formula II [e.g. 2-(bromomethyl)quinoline].
Abstract:
A process for the preparation of erythromycin compounds by alkylating 2’−O−acetyl−4”−O−formyl−11−oxo−8,9−anhydro− erythromycin A 6,9−hemiketal compound (1), characterized by reacting compound (1) with an alkylating agent in a mixed solvent consisting of 0.18 to 1.05 times as much water as compound (1) by equivalent and an organic solvent to thereby obtain a 2’ −O−acetyl−4”−O−formyl−11−oxo−12−alkoxy−8,9−anhydroerythro− mycin A 6,9−hemiketal compound (3).
Abstract:
2-Silyloxy-4,5,6,7-tetrahydrothieno[3,2-c]-pyridines represented by general formula (I), salts thereof, a process for producing the same, (wherein R , R and R each independently represent C1-C10 alkyl or aryl), 5-alkyl-2-silyloxy-4,5,6,7-tetrahydrothieno[3,2-c]pyridines represented by general formula (IV) and useful as intermediates in the synthesis of antithrombocytic agents or esterase inhibitors, and a process for producing the same, wherein R , R and R are each as defined above; R represents hydrogen, C2-C10 alkoxycarbonyl, C2-C10 aryl or C4-C10 cycloalkylcarbonyl; and R represents halogeno, C1-C4 alkyl or C1-C4 alkoxy.
Abstract:
PROBLEM TO BE SOLVED: To produce a 4-nitro ester compound in a high yield and in a high selectivity under mild conditions by reacting a nitroolefin compound with a ketene silyl acetal compound in the presence of a catalyst comprising the salt of an alkylpyridine compound with a superacid. SOLUTION: This method for producing a 4-nitro ester compound of formula IV comprises reacting a nitroolefin compound of formula II (R to R are each H, an alkyl or the like, or form a methylene chain between R and R ) (for example, nitroethylene) with a ketal silyl acetal compound of formula III (R and R are each H, an alkyl or the like, or form a methylene group between R and R ; R and R are each an alkyl, an aryl or a halogen; R is an alkyl, an alkenyl or the like) [for example, methyl(trimethylsily)dimethylketene acetal] in the presence of a 2-alkylpyridinium salt catalyst obtained by mixing a 2-alkylpyridine compound of formula I (R is an alkyl; R to R are each H, an alkyl or the like, or form methylene chains between R and R , between R and R , and between R and R , respectively) (for example, 2-methylpyridine) with a superacid.
Abstract:
PROBLEM TO BE SOLVED: To produce a 2,4,5-trifluoro-3-iodobenzoic acid and its ester which are useful as a material for 2,4,5-trifluoro-3-trifluoromethyl benzoic acids used as a starting material for production of antimicrobial and antiviral agents, easily and at a high yield. SOLUTION: This 2,4,5-trifluoro-3-iodobenzoic acid of formula I (R is an alkyl, cycloalkyl or aralkyl) is produced by making a 2,4,5-trifluoroiodobenzoic acid of formula II with a N-iodosuccinimide of formula III in the presence of trifluoromethane sulfonic acid. Furthermore, a 2,4,5-trifluoro-3-iodobenzoic ester of formula IV is obtained by reaction of a reactant mixture that contains a compound of formula I with an alcohol of the formula of R-OH.