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公开(公告)号:JP2002327130A
公开(公告)日:2002-11-15
申请号:JP2002005267
申请日:2002-01-11
Applicant: TOSOH CORP
Inventor: TOKUNAGA TAKUMI , ISHIGURO NORIHIKO , HORIE RYUICHI
Abstract: PROBLEM TO BE SOLVED: To provide a new fluorescent intercalative dye or the like which shows a large fluorescent enhancement upon intercalation into a double-stranded nucleic acid when used in detection of the nucleic acid, shows a great difference between the excitation wavelength and the fluorescence wavelength (i.e., has a large Stokes shift). SOLUTION: The purpose is attained by providing a compound represented by general formula 1, particularly e.g. compound 1 represented by formula 1A or a salt, hydrate, solvate or stereoisomer thereof, a method for producing these compounds and a nucleic acid probe obtained by bringing these compounds into contact with a nucleic acid or a nucleic acid probe obtained by chemically bonding these compounds to a single-stranded oligonucleotide.
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公开(公告)号:JP2000026476A
公开(公告)日:2000-01-25
申请号:JP19389698
申请日:1998-07-09
Applicant: TOSOH CORP , YOSHITOMI PHARMACEUTICAL
Inventor: YAMAMOTO TAKASHI , TOKUNAGA TAKUMI , ITO HIROYUKI , KONO KAZUHISA , HANAZAKI YASUAKI , KATSUURA KIMIO , SHINSAN HIROSHI , EGI YASUHARU , ISHIDA NAOMICHI , INOUE YOSHIHISA , YAMAUCHI KENJI
IPC: A61K31/695 , A61P3/06 , A61P9/10 , A61P43/00 , C07F7/10
Abstract: PROBLEM TO BE SOLVED: To obtain a new benzylamine derivative having squalene.epoxidase- inhibiting action and useful for the safe treatment of hyperlipemia, etc. SOLUTION: A new benzylamine derivative is a compound of formula I [R1 is a (substituted) phenyl or a heterocycle; L1 to L4 are each O, S, NR10 (R10 is H or a lower alkyl), or the like; R is H or a (halogen-substituted) lower alkyl; R3 to R6 are each H, a halogen, or the like; R7-R9 are each H or a lower alkyl], e.g. (E)-N-ethyl-N-(5-trimethylsilyl-2-penten-4-ynyl)-3-[2-(N'-methyl-N'- thiophen-3-ylmethyl-amino)ethyl]oxy-benzylamine. The compound of formula I is obtained e.g. by reacting an alcohol derivative of formula II with a phenol derivative of formula III in a solvent such as tetrahydrofuran in the presence of diethylazodicarboxylate and triphenylphosphine.
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公开(公告)号:JP2000026464A
公开(公告)日:2000-01-25
申请号:JP19389598
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: C07D409/12 , C07F7/10
Abstract: PROBLEM TO BE SOLVED: To obtain a new thiocarbamic acid ester derivative high in safety, having an antihypercholesterolemia activity and useful for treating arteriosclerosis or the like. SOLUTION: A compound of formula I [R1 is H, a lower alkyl or the like; R2 is H, a lower acyl or the like; R3 is a (substituted) phenyl or a heterocycle; R4 is H, a halogen, a lower alkyl or the like; R5 and R6 are each H or a lower alkyl, or they are linked with each other to form a ring; Y is C or Si; G1 to G3 are each CH or N; (m) and (n) are each 0 or 1; E is CR7R8 (R7 and R8 are each H or a lower alkyl); F is a carbonyl l or CR9R10 (R9 and R10 are each H or a lower alkyl)], for example, N-methyl-N-[3-[2-[N'-methyl-N'-3- thienylmethyl)amino]ethoxy]phenyl]thiocarbamic acid O-(5-trimethylsilylpyridin-2- yl)ester. Further, a compound of formula I is obtained by reacting a halogenated thioformate of formula II (V is a halogen) with a compound of formula III in a solvent such as tetrahydrofuran in the presence of a base.
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公开(公告)号:JP2000026455A
公开(公告)日:2000-01-25
申请号:JP19394498
申请日:1998-07-09
Applicant: TOSOH CORP
Inventor: YAMAMOTO TAKASHI , TOKUNAGA TAKUMI , ITO HIROYUKI , KONO KAZUHISA , HANAZAKI YASUAKI , KATSUURA KIMIO
IPC: C07D333/36
Abstract: PROBLEM TO BE SOLVED: To obtain a new 3-aminothiophene derivative useful as a synthetic intermediate, etc., of various physiologically active substances such as a medicine, an agrochemical, etc. SOLUTION: This new 3-aminothiophene derivative is a compound of formula I [R1, R2 are H, F, nitro, a lower alkyl, a alkoxy, a lower alkoxycarbonyl or a lower acryl; R3 is a lower alkyl; R4 to R7 are each H or a lower alkyl), e.g. N-(2-hydroxyethyl)-N-methyl-3-aminothiophene. Further, the compound of the formula I is obtained by reacting a 3-halothiophene derivative of formula II (X is a halogen) with an aminoalcohol derivative of formula III in an inert organic solvent such as tetrahydrofuran in the presence of a base such as triethylamine.
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公开(公告)号:JPH10251224A
公开(公告)日:1998-09-22
申请号:JP35658897
申请日:1997-12-25
Applicant: TOSOH CORP , GREEN CROSS CORP
Inventor: TOKUNAGA TAKUMI , TOKUHISA KENJI , ITO HIROYUKI , YAMAMOTO TAKASHI , KATSUURA KIMIO , ISHIDA NAOMICHI , AIDA MASAKI , MATSUNO SUMIO , INOUE YOSHIHISA , YAMAUCHI KENJI
IPC: C07D239/26 , A61K31/165 , A61K31/215 , A61K31/275 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4433 , A61K31/505 , A61K31/695 , A61P3/06 , A61P9/10 , A61P43/00 , C07C333/02 , C07C333/08 , C07D209/08 , C07D209/34 , C07D209/44 , C07D209/46 , C07D213/74 , C07D277/20 , C07D277/28 , C07D277/42 , C07D285/08 , C07D285/10 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/36 , C07D333/38 , C07D409/12 , C07D417/12
Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound useful as an agent for alleviating hypercholesterolemia or an agent for hyperlipemia. SOLUTION: This compound is shown by formula I [R is trifluoromethyl, phenyl, etc.; R1 is H or a lower alkyl; (1) is 0 or 1; X and Z are each carbonyl, etc.; (m) is 0 or 1; (n) is 1 or 2; Y is O, S, etc.; Q is ethylene, trimethylene, etc.; R2 is H or a lower alkyl; A is a group of formula II (R3 and R4 are each H, a halogen, etc.)] such as N-(3-thienyl)-N-methyl-3-(3-aminophenoxy) propylamine. The compound is obtained by reacting a halogenated thioformate of formula III (V is a halogen) with an amine of formula IV in an equimolar amounts or in a little excessive amount of either of the compounds in the presence or absence of a base (sodium hydroxide) in a solventless state or in a solvent (methanol) at -80 to 100 deg.C for several minutes to 24 hours.
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公开(公告)号:JPH10204057A
公开(公告)日:1998-08-04
申请号:JP1248597
申请日:1997-01-27
Applicant: TOSOH CORP , GREEN CROSS CORP
Inventor: TOKUNAGA TAKUMI , ITO HIROYUKI , KONO KAZUHISA , YAMAMOTO TAKASHI , KATSUURA KIMIO
IPC: C07C215/50 , C07C233/25 , C07C255/36 , C07C329/02 , C07F7/12
Abstract: PROBLEM TO BE SOLVED: To simply and economically produce the subject derivative, having a readily modifiable substituent group and useful as a production intermediate for physiologically active substances by reacting a phenol compound with a halogenothiocarbamating agent. SOLUTION: This compound is represented by formula I (R is a tri-lower alkylsilyl, a group represented by formula II (R1 is a lower alkoxy, cyano, a lower alkoxycarbonyl, etc.), etc.; V is a halogen), e.g. 4-(2-amino-1,1- dimethylethyl)phenoxy-tert-butyldimethylsilane. The objective derivative is preferably produced by reacting, e.g. a phenol compound represented by formula III with a halogenothiocarbamating agent, e.g. thiophosgene in the presence of a base in or without a solvent at -10 to +10 deg.C for several min to 24hr.
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37.
公开(公告)号:JPH05186426A
公开(公告)日:1993-07-27
申请号:JP35950091
申请日:1991-12-30
Applicant: TOSOH CORP
Inventor: TOKUNAGA TAKUMI , TAKASU YASUHITO , WATANABE HIROYUKI , TSUZUKI KENJI , IDE TERUHIKO
IPC: A01N43/42 , C07D217/26 , C07D405/04
Abstract: PURPOSE:To obtain a new tetrahydroisoquinolone derivative showing sufficient effects and no problems in terms of environmental toxicity in the case of use as a fungicide. CONSTITUTION:Compounds of formula I and formula II [R is 1-5C alkyl, 2-5C alkenyl or 2-5C alkynyl; R to R are H, 1-10C alkyl, 3-10C alkenyl, 2-10C alkynyl, 1-10C alkoxy, 2-10C alkenyloxy, 2-10C alkynyloxy, benzyloxy, OH, halogenated alkyl, NH2, amino substituted or disubstituted with 1-4C alkyl, phenyl, halogen, group of formula III or formula IV (R is 1-10C alkyl; R and R are H or R ) or R and R or R and R are bonded to form group formula V (m is 1 or 2) or formula VI] such as 3-(4-t-butylphenyl)-4-hydroxycarbonyl-2- methyl-1-oxo-1,2,3,4-tetrahydroisoquinoline. The compound of formula I is obtained by reacting an imine derivative of formula Vll with homophthalic anhydride in a solventless state or in the presence of a solvent preferably at 0-100 deg.C.
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38.
公开(公告)号:JPH03258771A
公开(公告)日:1991-11-19
申请号:JP5653290
申请日:1990-03-09
Applicant: TOSOH CORP
Inventor: TOKUNAGA TAKUMI , SAKKA YASUO , WATANABE HIROYUKI , TSUZUKI KENJI
IPC: C07D271/06 , A01N43/82 , A01N43/836
Abstract: NEW MATERIAL:A compound of formula I [X is 1-4C alkyl, hydroxy, 1-4C alkoxy, amino, nitro, halogen; X is H, halogen; X is not H when X is 4-amino; R is H, 1-4C alkyl, COOR (R is 1-4C alkyl), phenyl, etc.; Y is H, 1-6C alkyl, 3-4C alkenyl, 3-4C alkinyl, 2-6C alkyl sustitutable at O]. EXAMPLE:5-Methyl-3-(4-methylphenyl sulfonylamino)-1,2,4-oxadiazole. USE:A herbicide. The compound of formula I exhibits an excellent herbicidal activity against upland or rice field weeds such as E chinochloa, Cyperus and Scirpus and has high safety to crops. PREPARATION:A hydroxy guanidine derivative of formula II is reacted with an acid halide of formula III (X is halogen) or an acid anhydride of formula IV to provide the compound of formula I.
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公开(公告)号:JPH03258703A
公开(公告)日:1991-11-19
申请号:JP5653390
申请日:1990-03-09
Applicant: TOSOH CORP
Inventor: TOKUNAGA TAKUMI , SAKKA YASUO , WATANABE HIROYUKI , TSUZUKI KENJI
IPC: A01N43/836 , A01N43/82
Abstract: PURPOSE:To obtain a herbicide capable of controlling various weeds from the pre-sprouting stage to growing stage and having high safety to crops by using a sulfonamide derivative having oxadiazole ring and its salt as an active component. CONSTITUTION:The objective herbicide contains a compound of formula [X is alkyl, OH, alkoxy, NH2, NO2 or halogen; X is H or halogen; R is H, alkyl, COOR (R is alkyl), phenyl, benzyl, etc.; Y is H, alkyl, alkenyl, alkynyl, etc.) and its salt (e.g. salts produced by NaOH, ammonia, etc.] as an active component. The herbicide can be used in combination with other agricultural chemicals such as fungicide, insecticide, herbicide and plant growth regulator. Especially, the labor can be saved and the herbicidal spectrum is expected to be expanded by the mixed use with other herbicide. The rate of application is 10-500g of the active component per 10 are.
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公开(公告)号:JPH02215777A
公开(公告)日:1990-08-28
申请号:JP3622289
申请日:1989-02-17
Applicant: TOSOH CORP
Inventor: TOKUNAGA TAKUMI , KAGAWA TAKUMI , WATANABE HIROYUKI , TSUZUKI KENJI
IPC: C07D307/12 , A01N43/08
Abstract: NEW MATERIAL:An optically active lactic ester derivative expressed by formula I [R is 1-3C alkyl, benzyl or phenyl (able to be 1-3 substituted by methyl, isopropyl, methoxy, nitro or amino, etc.)]. EXAMPLE:(2S)-tetrahydrofurfuryl 2-p-toluenesulfonyloxy propionate. USE:Producing intermediate of physics or agricultural chemicals, etc. PREPARATION:Alkylsulfonic acid halide expressed by formula II (X is halogen) is reacted with optically active (2S)-tetrahydrofurfuryl 2-hydroxy propionate to obtain the compound expressed by formula I.
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