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1. 发明专利

JP2001081086A PRODUCTION OF 1,4-BENZODIOXANES 失效
公开(公告)号：JP2001081086A
公开(公告)日：2001-03-27
申请号：JP25715299
申请日：1999-09-10
申请人： DAISO CO LTD
发明人： FURUKAWA YOSHIRO , KITAORI KAZUHIRO , YOSHIMOTO HIROSHI , ODERA JUNZO
IPC分类号： C07D319/20 , C07B53/00
摘要： PROBLEM TO BE SOLVED: To provide a method for producing 1,4-benzodioxanes, capable of producing the benzodioxane compound which is useful as an intermediate for medicaments, such as a cardiovascular disease remedy and a psychoneurotic disease remedy, having α- and β-adrenaline antagonistic actions in a high yield, by using a specific diol compound as a starting material and carrying out reactions without isolating the formed reaction intermediates. SOLUTION: This method for producing 1,4-benzodioxanes comprises converting hydroxy groups of a diol compound of formula I (R1 is a hydroxy- protecting group; R2 to R4 are H, a halogen, hydroxy or the like) into an eliminating group in the presence of a base or a fluoride compound to form a compound of formula II (B is an eliminable group), them eliminating the protecting group R1 from the formed compound and simultaneously carrying out ring closure reaction to form a 1,4-benodioxane compound of formula III (A is hydroxy, sulfonate or the like) [for example, (R)-8-methyl-2-tosyloxymethyl-1,4- benzodioxane], wherein one-pot reaction is carried out by adding only necessary reaction reagents to the diol compound without isolating any intermediates formed in the course of the above reactions.

2. 发明专利

JPH05170682A PRODUCTION OF OPTICALLY ACTIVE LINALOOL AND ITS INTERMEDIATE 失效
公开(公告)号：JPH05170682A
公开(公告)日：1993-07-09
申请号：JP24740291
申请日：1991-09-26
申请人： DAISO CO LTD
发明人： ODERA JUNZO , SHIMIZU YASUMI
IPC分类号： B01J27/16 , B01J31/12 , C07B61/00 , C07C29/56 , C07C33/02
摘要： PURPOSE:To readily produce the subject compound of high purity by synthesizing an optically active glycol derivative through a reaction of a specified optically active compound in the presence of a specified catalyst, reacting a formamide acetal derivative, etc., therewith and subsequently carrying out hydrolysis, etc. CONSTITUTION:A derivative of formula II is synthesized by a ring-opening addition reaction between a compound of formula I (* denotes an asymmetric carbon atom) and an alcohol of formula R OH (R is C6H5CH2-, CH2=CH-CH2-, etc.) in the presence of a catalyst composed of a thermal condensate between an organotin compound of formula R aSnX4-a, formula R bSnOc, etc., (R is a 1-12C alkyl, alkenyl, etc., which respectively may have a substituent; X is a halogen, an alkoxy, etc.; a is 1-4; b is 1-2; c is 3/2 or 1 respectively in the case of b=1 or b=2) and a phosphoric acid ester of formula (R O)3P=O (R is H, an alkenyl, etc.). Another derivative of formula III (R and R are methyl, ethyl etc.) is reacted with the synthesized formula II and an acid anhydride of formula (R CO)2O (R is methyl, ethyl, etc.) is subsequently reacted therewith to obtain a compound of formula IV. The compound of formula IV is subjected to hydrolysis, etc., in the presence of a metal catalyst, thus obtaining the objective compound of formula (D).

3. 发明专利

JPS6485935A PRODUCTION OF HYDROXY COMPOUND 失效
公开(公告)号：JPS6485935A
公开(公告)日：1989-03-30
申请号：JP24568287
申请日：1987-09-28
申请人： DAISO CO LTD
发明人： ODERA JUNZO , NAKADA TETSUYA
IPC分类号： C07B61/00 , B01J31/12 , C07B31/00 , C07B41/02 , C07B51/00 , C07C27/00 , C07C29/10 , C07C29/132 , C07C31/125 , C07C33/02 , C07C33/22 , C07C35/18 , C07C67/00
摘要： PURPOSE:To conduct the selective elimination of the protecting group from the title compound having hydroxyl groups protected with tetrahydropyranyl or silyl groups, by using a thermal condensate of a specific organotin compound with an alkyl phosphate as a catalyst. CONSTITUTION:Using, as a catalyst, a thermal condensate from a compound selected from formulas I-III (R is 1-12C alkyl, alkenyl, cycloalkyl, aryl, aralkyl which may be substituted; X is halogen, alkoxy, aryloxy, acyloxy, residue of partial phosphate ester; a is integer of 1-4; c=3/2 in b=1, c=1 in b=2; the compound of formula II may form a complex with the compound of formula III) and an alkyl phosphate, an organic compound containing a structural unit of the formula IV (Y is OH-protecting group such as tetrahydropyranyl or silyl), especially a compound sensitive to acid is deprotected selectively to liberate the subject hydroxyl compound in high efficiency.

4. 发明专利

JP2003206282A METHOD FOR PRODUCING OXAZOLIDIN-2-ONE DERIVATIVE 审中-公开
公开(公告)号：JP2003206282A
公开(公告)日：2003-07-22
申请号：JP2002000387
申请日：2002-01-07
申请人： DAISO CO LTD
发明人： ODERA JUNZO , FURUKAWA YOSHIRO , YOSHIMOTO HIROSHI
IPC分类号： C07D263/20
摘要： PROBLEM TO BE SOLVED: To provide an industrial method for producing an oxazolidin-2-one derivative. SOLUTION: This method for producing the oxazolidin-2-one derivative of general formula (3) (wherein, R 1 means hydrogen atom, an alkyl group, an alkoxy-substituted alkyl group or the like; and R 2 means hydrogen atom, an alkyl group, a substituted or an unsubstituted aralkyl group or the like) is carried out as follows. An epoxy compound of general formula (1) is reacted with a carbamate derivative or a urea derivative in the presence of a cesium salt. COPYRIGHT: (C)2003,JPO

5. 发明专利

JPH1160530A PRODUCTION OF OPTICALLY ACTIVE BETA-ALKOXYALCOHOL 失效
公开(公告)号：JPH1160530A
公开(公告)日：1999-03-02
申请号：JP31496797
申请日：1997-11-17
申请人： DAISO CO LTD
发明人： MATSUI SHOHEI , FURUKAWA YOSHIRO , KITAORI KAZUHIRO , YOSHIMOTO HIROSHI , ODERA JUNZO
IPC分类号： B01J27/232 , C07B61/00 , C07C41/03 , C07C43/13 , C07C43/178 , C07C43/196 , C07C43/23 , C07C43/253 , C07C67/29 , C07C67/31 , C07C69/14 , C07C69/67 , C07D317/20
摘要： PROBLEM TO BE SOLVED: To obtain on high yield the subject compound useful as a medicine or an intermediate for synthesizing medicines, by reaction of fan optically active epoxide or optically active epoxide precursor with an excess amount of an aliphatic alcohol in the presence of a fluoride. SOLUTION: This compound is obtained by reaction of an optically active epoxide of formula I (R to R are each H, a halogen or the like)(pref. propylene oxide) or an optically active epoxide precursor of formula II (X is a group eliminable when reacted with the alcohol described below)(e.g. 2-chloroethanol) with an excess amount of an aliphatic alcohol (pref. methanol) in the presence of a fluoride (e.g. sodium fluoride) at 15-160 deg.C. In the above process, as necessary, addition of a weak base (e.g. sodium bicarbonate) as an acid trapping agent accelerates the reaction and also enables the amount of the fluoride to be used to be reduced. It is preferable that the amounts of the aliphatic alcohol, the fluoride and the trapping agent to be used are 1.5-10 equivalents, 0.001-10 equivalents and 1-3 equivalents based on the reaction substrate, respectively.

6. 发明专利

JPH1160529A PRODUCTION OF ETHER 失效
公开(公告)号：JPH1160529A
公开(公告)日：1999-03-02
申请号：JP31496597
申请日：1997-11-17
申请人： DAISO CO LTD
发明人： MATSUI SHOHEI , FURUKAWA YOSHIRO , KITAORI KAZUHIRO , YOSHIMOTO HIROSHI , ODERA JUNZO
IPC分类号： C07D317/20 , C07C41/03 , C07C43/178 , C07C43/23 , C07C43/253
摘要： PROBLEM TO BE SOLVED: To obtain in high yield an ether useful as an medicine or an intermediate for synthesizing medicines, by reaction of an epoxide or epoxide with an alcohol in the presence of a fluoride in a specific organic solvent. SOLUTION: This ether is obtained by reaction of an epoxide of formula I (R to R are each H, a halogen or the like)(pref. propylene oxide) or an epoxide precursor of formula II (X is a group eliminable when reacted with the alcohol described below)(e.g. 2-chloroethanol) with an alcohol (pref. methanol or the like) in the presence of a fluoride (e.g. sodium fluoride) in a solvent selected from aprotic polar solvents (pref. N,N-dimethylformamide or the like), nitrile-based solvents (pref. acetonitrile) and aromatic solvents (pref. benzene or the like) pref. at 15-160 deg.C; wherein the amounts of the alcohol and the fluoride to eve used are pref. 0.5-10 equivalents and 0.001-10 equivalents based on the reaction substrate, respectively.

7. 发明专利

JPH03251577A STEREOCHEMICAL INVERSION OF OPTICALLY ACTIVE STYRENE OXIDE AND PRODUCTION OF OPTICALLY ACTIVE GLYCOL DERIVATIVE 失效
公开(公告)号：JPH03251577A
公开(公告)日：1991-11-11
申请号：JP4690490
申请日：1990-02-27
申请人： DAISO CO LTD
发明人： ODERA JUNZO , MIURA KATSUTO
IPC分类号： C07D303/04 , B01J31/12 , C07B53/00 , C07B61/00 , C07C33/46 , C07C41/03 , C07C43/178 , C07C309/66 , C07C309/73 , C07D301/00 , C07D301/02 , C07D301/24 , C07D301/26
摘要： PURPOSE:To obtain the glycol derivative of formula VI useful as a raw material for pharmaceuticals and agricultural chemicals, etc., in high yield and purity by producing an optically active glycol derivative from an optically active styrene oxide in the presence of a specific catalyst and reacting the obtained derivative with a sulfonic acid halide, etc. CONSTITUTION:A compound of formula IV (Ph is phenyl; * represents asymmetric carbon) is produced by the ring-opening addition reaction of an alcohol of formula R'OH to an optically active styrene oxide in the presence of a catalyst composed of a thermal condensation reaction product of an organic tin compound selected from the group of formula I (R' is 1-12C alkyl, etc.; X is halogen, etc.; a is 1-4), formula II (b is 1 or 2; C is 3/2 when b is 1, and C is 1 when b is 2), etc., with a compound of formula III (R'' is H, >=2C alkyl, etc.), etc. The objective compound of formula VI can be produced by reacting the compound of formula IV with a sulfonic acid halide in the presence of a base and reacting the resultant compound of formula V (R is tosyl, mesyl, etc.) in the presence of an acidic catalyst, a metallic catalyst or a mixture of an acidic catalyst and a metallic catalyst.

8. 发明专利

JP2006111615A Method for producing imidazopyran derivative 有权
标题翻译：生产咪唑衍生物的方法
公开(公告)号：JP2006111615A
公开(公告)日：2006-04-27
申请号：JP2005262564
申请日：2005-09-09
申请人： Daiso Co Ltd , ダイソー株式会社
发明人： ODERA JUNZO , ORITA AKIHIRO
IPC分类号： C07D498/04 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a new method for producing an imidazopyran derivative. SOLUTION: In this new method for producing an imidazopyran, dinitroimidazol and 2,3-epoxy-1-propanol are used as starting substances to produce an imidazopyran derivative represented by formula (9) (wherein R 1 is a 1-3C alkyl, an aryl, an aryl-substituted 1-3C alkyl, a halogen atom or H) through a process comprising five steps. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：提供一种生产咪唑并吡喃衍生物的新方法。解决方案：在该新的咪唑并吡喃生产方法中，使用二硝基咪唑和2,3-环氧-1-丙醇作为起始物质，制备由式（9）表示的咪唑并吡喃衍生物（其中R 通过包括五个步骤的方法，SP>是1-3C烷基，芳基，芳基取代的1-3C烷基，卤素原子或H）。版权所有（C）2006，JPO＆NCIPI

9. 发明专利

JPH1059955A 2-OXO-3-OXIBICYCLO(3,1,0)HEXANE DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPH1059955A
公开(公告)日：1998-03-03
申请号：JP12085097
申请日：1997-05-12
申请人： DAISO CO LTD
发明人： MIKAMI MASAFUMI , FURUKAWA YOSHIRO , ODERA JUNZO , YOSHIMOTO HIROSHI
IPC分类号： C07D307/93 , B01J27/12 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To produce a 2-oxo-3-oxabicylo[3,1,0]hexane derivative containing partially new one useful as an intermediate for a medicine and a physiologically active substance by reacting a specific epoxy compound with an analogue of malonic acid under a mild condition. SOLUTION: This 2-oxo-3-oxabicylo[3,1,0]hexane derivative is produced by reacting an epoxy compound of formula I [R is a halogen or OSO2 R (R is an alkyl or phenyl)] with an analogue of malonic acid in the presence of a metallic salt of fluorine. Epichlorohydrin, glycidyl methanesulfonate, glycidyl trifluoromethanesulfonate, etc., are preferably used as the epoxy compound of formula I. A malonic acid dialkyl ester, malonic acid diaryl ester, etc., are preferable as the analogue of the malonic acid in the method for producing 2-oxo-3-oxabicylo[3,1,0]hexane derivative. An alkali metal salt of the fluorine is preferable as the metallic salt of the fluorine. The 2-oxo-3- oxabicylo[3,1,0]hexane derivative of formula II in which the R of the formula II is, for example, phenyloxycarbonyl is the new one is the 2-oxo-3- oxabicylo[3,1,0]hexane derivative of formula II (R is an alkyloxycarbonyl, an aryloxycarbonyl, etc.).

10. 发明专利

JP2000281619A PRODUCTION OF 1-ACYLOXY-3-HALOGENO-2-PROPANOL AND EPIHALOHYDRIN AND 1-ACYLOXY-3-HALOGENOPROPANE-2- SULFONATE 失效
公开(公告)号：JP2000281619A
公开(公告)日：2000-10-10
申请号：JP9111599
申请日：1999-03-31
申请人： DAISO CO LTD
发明人： ODERA JUNZO , FURUKAWA YOSHIRO , YOSHIMOTO HIROSHI
IPC分类号： C07D301/02 , B01J31/02 , C07B61/00 , C07C67/03 , C07C67/08 , C07C69/63 , C07C309/66 , C07D303/08
摘要： PROBLEM TO BE SOLVED: To industrially advantageously synthesize the subject compound useful as a synthetic intermediate for a medicine, agrochemical, etc., by reacting a specific propanediol with an acylating agent in the presence of a tin-based catalyst. SOLUTION: (A) A 3-halogeno-1,2-propanediol of formula I (X is a halogen) is treated with (C) an acylating agent (preferably a vinyl carboxylate, a carboxylic acid anhydride, especially vinyl acetate) in the presence of (B) a tin-based catalyst (preferably distannoxane or stanoxide) to give a compound of formula II [R1 is a (substituted) alkyl or aryl]. For example, preferably the reaction is carried out by using 3-chloro-1,2-propanediol, etc., as the component A, >=1 equivalent based on the component A of the component C and 0.01-50 mol% of the component B at a temp. of -78 deg.C to the reflux temperature of the solvent.

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