公开(公告)号：FR2753966B1

公开(公告)日：2003-10-31

申请号：FR9712024

申请日：1997-09-26

Applicant: TOSOH CORP

Inventor： KATSUURA KIMIO ,  IRINO SHIGEAKI ,  TOKUDA AKIRA

IPC: C07C227/34 ,  C07C227/40 ,  C07C227/42 ,  C07C229/36

Abstract: A method for producing an optically active amino acid or derivative thereof having a high optical purity from an optically active amino acid comprising optical isomers or derivative thereof, which comprises any one of processes (A), (B), and (C), wherein the process (A) comprises the steps: (1) previously preparing an optically active amino acid or derivative thereof having an optical purity higher than a convergent value of a mutual solubility of the optical isomers and (2) crystallizing the optically active amino acid or the derivative thereof that exists in excess, said convergent value being a ratio of the desired optical isomer in the optical isomers dissolved in a mother liquor in which crystals of a racemate and an optically active compound coexist at equilibrium (the optical purity in a mother liquor). The processes (B) and (C) are described in the specification.

公开(公告)号：ES2111197T3

公开(公告)日：1998-03-01

申请号：ES94106146

申请日：1994-04-20

Applicant: TOSOH CORP

Inventor： HANASAKI YASUAKI ,  WATANABE HIROYUKI ,  KATSUURA KIMIO ,  FUJIWARA MASATOSHI ,  IDE TERUHIKO

IPC: A01N43/82 ,  A01N43/832 ,  A01N47/06 ,  A01N47/18 ,  C07D285/10

Abstract: Disclosed is (a) 1,2,5-thiadiazole derivatives represented by the following formulae [I] or [III]: wherein X and Y are the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, a nitro group, a trifluoromethyl group, a carboxyl group, an alkoxycarbonyl group having from 1 to 5 carbon atoms, a naphthyl group or a tetrahydronaphthyl group; and A represents an alkyl group having from 1 to 6 carbon atoms, -C(=O)OR , -C(=O)NR R , a phenyl group which may be substituted by at least one of an alkyl group having from 1 to 6 carbon atoms and an alkoxy group having from 1 to 4 carbon atoms, -CHR C(=O)R or -C(=O)R , in which R represents an alkyl group having from 1 to 6 carbon atoms, R and R are the same or different and each represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms, R represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, R represents an alkoxy group having from 1 to 4 carbon atoms or an amino group which may be substituted by at leaset one of an alkyl group having from 1 to 4 carbon atoms and a phenyl group which may be substituted by at least one halogen atom, and R represents an alkyl group having from 1 to 6 carbon atoms, (b) a process for producing the compound represented by formula [I] and (c) an agricultural and horticultural fungicide comprising the compound represented by formula [III].

公开(公告)号：FR2753966A1

公开(公告)日：1998-04-03

申请号：FR9712024

申请日：1997-09-26

Applicant: TOSOH CORP

Inventor： KATSUURA KIMIO ,  IRINO SHIGEAKI ,  TOKUDA AKIRA

IPC: C07C227/34 ,  C07C227/40 ,  C07C227/42 ,  C07C229/36

Abstract: Three methods (A)-(C) are claimed for preparing aminoacids (AA) and their hydrochlorides in optically pure form. Method (A) involves preparing AA having an optical purity above the convergence value (CV) of the mutual solubility of the optical isomers, where CV is the fraction of the desired optical isomer in the mixture of isomers in a mother liquor in which racemate and optical isomers co-exist in equilibrium. The optical isomer of the AA in excess above CV is then crystallised out. Method (B) involves crystallising an optically active AA at a pH around the isoelectric point, reducing the pH of the mother liquor to 1 or less and recovering the resulting crystals. Method (C) involves: mixing an optically active AA ester in aqueous solution with an N-substituted - alpha -L-aspartyl-L-phenyl alanine alkyl ester of formula (I); extracting the addition product with a water-immiscible organic solvent; washing the organic solution is with an aqueous acid; and decomposing the organic solution with an acid to isolate the pure D-AA in aqueous acid solution. R1 = optionally substituted phenyl; R2 = aliphatic oxycarbonyl or optionally substituted benzyloxycarbonyl; R3 = alkyl.

公开(公告)号：NL1007126A1

公开(公告)日：1998-03-31

申请号：NL1007126

申请日：1997-09-26

Applicant: TOSOH CORP

Inventor： KATSUURA KIMIO ,  IRINO SHIGEAKI ,  TOKUDA AKIRA

IPC: C07C227/34 ,  C07C227/40 ,  C07C227/42 ,  C07C229/36 ,  C07C227/30

Abstract: A method for producing an optically active amino acid or derivative thereof having a high optical purity from an optically active amino acid comprising optical isomers or derivative thereof, which comprises any one of processes (A), (B), and (C), wherein the process (A) comprises the steps: (1) previously preparing an optically active amino acid or derivative thereof having an optical purity higher than a convergent value of a mutual solubility of the optical isomers and (2) crystallizing the optically active amino acid or the derivative thereof that exists in excess, said convergent value being a ratio of the desired optical isomer in the optical isomers dissolved in a mother liquor in which crystals of a racemate and an optically active compound coexist at equilibrium (the optical purity in a mother liquor). The processes (B) and (C) are described in the specification.

公开(公告)号：DE69406836D1

公开(公告)日：1998-01-02

申请号：DE69406836

申请日：1994-04-20

Applicant: TOSOH CORP

Inventor： HANASAKI YASUAKI ,  WATANABE HIROYUKI ,  KATSUURA KIMIO ,  FUJIWARA MASATOSHI ,  IDE TERUHIKO

IPC: A01N43/82 ,  A01N43/832 ,  A01N47/06 ,  A01N47/18 ,  C07D285/10

Abstract: Disclosed is (a) 1,2,5-thiadiazole derivatives represented by the following formulae [I] or [III]: wherein X and Y are the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, a nitro group, a trifluoromethyl group, a carboxyl group, an alkoxycarbonyl group having from 1 to 5 carbon atoms, a naphthyl group or a tetrahydronaphthyl group; and A represents an alkyl group having from 1 to 6 carbon atoms, -C(=O)OR , -C(=O)NR R , a phenyl group which may be substituted by at least one of an alkyl group having from 1 to 6 carbon atoms and an alkoxy group having from 1 to 4 carbon atoms, -CHR C(=O)R or -C(=O)R , in which R represents an alkyl group having from 1 to 6 carbon atoms, R and R are the same or different and each represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms, R represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, R represents an alkoxy group having from 1 to 4 carbon atoms or an amino group which may be substituted by at leaset one of an alkyl group having from 1 to 4 carbon atoms and a phenyl group which may be substituted by at least one halogen atom, and R represents an alkyl group having from 1 to 6 carbon atoms, (b) a process for producing the compound represented by formula [I] and (c) an agricultural and horticultural fungicide comprising the compound represented by formula [III].

公开(公告)号：NL1007126C2

公开(公告)日：2003-01-08

申请号：NL1007126

申请日：1997-09-26

Applicant: TOSOH CORP

Inventor： KATSUURA KIMIO ,  IRINO SHIGEAKI ,  TOKUDA AKIRA

IPC: C07C227/34 ,  C07C227/40 ,  C07C227/42 ,  C07C229/36

公开(公告)号：DE69406836T2

公开(公告)日：1998-06-25

申请号：DE69406836

申请日：1994-04-20

Applicant: TOSOH CORP

Inventor： HANASAKI YASUAKI ,  WATANABE HIROYUKI ,  KATSUURA KIMIO ,  FUJIWARA MASATOSHI ,  IDE TERUHIKO

IPC: A01N43/82 ,  A01N43/832 ,  A01N47/06 ,  A01N47/18 ,  C07D285/10

Abstract: Disclosed is (a) 1,2,5-thiadiazole derivatives represented by the following formulae [I] or [III]: wherein X and Y are the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group having from 1 to 6 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, a nitro group, a trifluoromethyl group, a carboxyl group, an alkoxycarbonyl group having from 1 to 5 carbon atoms, a naphthyl group or a tetrahydronaphthyl group; and A represents an alkyl group having from 1 to 6 carbon atoms, -C(=O)OR , -C(=O)NR R , a phenyl group which may be substituted by at least one of an alkyl group having from 1 to 6 carbon atoms and an alkoxy group having from 1 to 4 carbon atoms, -CHR C(=O)R or -C(=O)R , in which R represents an alkyl group having from 1 to 6 carbon atoms, R and R are the same or different and each represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms, R represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, R represents an alkoxy group having from 1 to 4 carbon atoms or an amino group which may be substituted by at leaset one of an alkyl group having from 1 to 4 carbon atoms and a phenyl group which may be substituted by at least one halogen atom, and R represents an alkyl group having from 1 to 6 carbon atoms, (b) a process for producing the compound represented by formula [I] and (c) an agricultural and horticultural fungicide comprising the compound represented by formula [III].

公开(公告)号：JP2000026452A

公开(公告)日：2000-01-25

申请号：JP19389498

申请日：1998-07-09

Applicant: TOSOH CORP ,  YOSHITOMI PHARMACEUTICAL

Inventor： TOKUNAGA TAKUMI ,  YAMAMOTO TAKASHI ,  ITO HIROYUKI ,  KONO KAZUHISA ,  HANAZAKI YASUAKI ,  KATSUURA KIMIO ,  SHINSAN HIROSHI ,  EGI YASUHARU ,  ISHIDA NAOMICHI ,  INOUE YOSHIHISA ,  YAMAUCHI KENJI

IPC: C07D333/20 ,  A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/495 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D333/28 ,  C07D409/12

Abstract: PROBLEM TO BE SOLVED: To obtain a new ethylenediamine derivative having a higher safety compared with conventional medicines, a inhibitory activity to a squalene epoxidase originating from a mammalian animal and an excellent anti- cholesterol activity, and useful as an anti-hyperlipidemic agent, etc. SOLUTION: This new ethylenediamine derivative is a compound of formula I [R1, R2 are each H, a lower alkyl or a lower cyclic alkyl; R3 is H, a lower alkyl or a lower acryl; R2 and R3 form a ring by bonding each other; R4 is a (substituted) thienyl; A is formula II (R5 is H, a halogen, a lower alkoxy or the like; G1 to G3 are each CH or N); (m), (n) are each 0, 1; E is carbonyl or the like; F is carbonyl or the like; Z1 to Z4 are each CH or N; X is O or S], e.g. N-[3-[2-[N'-methyl-N'-(3-thienylmethyl)amino]ethylamino]phenyl]-N- methylthiocarbamic acid O-(4-tert-butylphenyl)ester. Further, the compound of formula I is obtained by reacting a halogenated formate derivative of formula III (V is a halogen) with a compound of formula IV.

公开(公告)号：JPH0797377A

公开(公告)日：1995-04-11

申请号：JP25977293

申请日：1993-10-18

Applicant: TOSOH CORP

Inventor： HANAZAKI YASUAKI ,  FUJIWARA MASAHISA ,  IDE TERUHIKO ,  WATANABE HIROYUKI ,  KATSUURA KIMIO

IPC: C07D285/10 ,  A01N43/832 ,  A01N47/06 ,  A01N47/12

Abstract: PURPOSE:To obtain the subject derivative useful for exterminating and eradicting injury of blight caused by a wide range of various microorganisms, having excellent antimicrobial activity, excellent bacteridal potency especially on pathogenic germs of plants. CONSTITUTION:The objective derivative of formula I [X and Y are H, a halogen, a 1-6C alkyl, a 1-4C alkoxy, hydroxy, nitro, carboxyl or a 1-4C alkoxy- substituted carbonyl; A is a 1-6C alkyl, a 1-6C alkyl, 1-4C alkoxy-substituted phenyl, C(=O)OR1 (R1 is a 1-6C alkyl), C(=W)NR2R3 (W is O or S; R2 and R3 are H, a 1-4C alkoxy-substituted 1-6C alkyl or a 1-4C alkoxy), group of formula II (n is 0-2; R to R each is H, a halogen, a 1-6C alkyl or a 1-4C alkoxy) or R2 and R3 are mutually bonded to form group of formula III (n is 0-2; E is CH2 or O; R and R are H, a 1-6C alkyl), CHR9COR10(R9 is H or a 1-4C alkyl; R10 is a 1-4C alkoxy or NR2R3), C(=O)R11 (R11 is a 1-6C alkyl)].

公开(公告)号：JPH01102058A

公开(公告)日：1989-04-19

申请号：JP25832887

申请日：1987-10-15

Applicant: TOSOH CORP

Inventor： AWANO YUTAKA ,  TSUZUKI KENJI ,  KATSUURA KIMIO

IPC: C07C329/02 ,  C07C67/00 ,  C07C325/00

Abstract: PURPOSE:To obtain the title compound useful as an intermediate for pharmaceuticals, etc., in high yield and purity, by reacting 5,6,7,8-tetrahydro-2- naphthol with thiophosgene in the presence of a sulfur-containing inorganic reducing agent such as sulfur dioxide gas or hydrogen sulfide gas. CONSTITUTION:2-(5,6,7,8-Tetrahydronaphthoxy)-chlorothioformate is produced by reacting (A) 5,6,7,8-tetrahydro-2-naphthol with (B) thiophosgene in the presence of a dehydrohalogenation reagent (e.g. NaOH) and at least one kind of additive selected from sulfur dioxide gas, hydrogen sulfide gas and an alkali metal sulfide (e.g. Na2S and K2S) dissolved in the reaction mixture. The amount of the additive is 0.005-1mol., preferably 0.02-0.1mol. per 1mol. of the component A.