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11. 发明专利

JP2004099481A Method for producing trifluoromethyl-substituted 2-alkoxyacetophenone derivative 有权
标题翻译：生产三氟甲基取代的2-烷氧基乙烯酮衍生物的方法
公开(公告)号：JP2004099481A
公开(公告)日：2004-04-02
申请号：JP2002261160
申请日：2002-09-06
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO , OTSUKA TAKASHI , UEDA KOJI
IPC分类号： C07D317/16 , C07B61/00 , C07C45/57 , C07C45/59 , C07C49/84
CPC分类号： Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing a trifluoromethyl-substituted 2-alkoxyacetoxyphenone derivative used as an important intermediate for medicines and agrochemicals. SOLUTION: This method for producing the trifluoromethyl-substituted 2-alkoxyacetoxyphenone derivative comprises brominating a trifluoromethyl-substituted acetophenone with Br 2 in the presence of an alkylenediol, subjecting the obtained brominated acetal to a substitution reaction with a metal alkoxide, and then hydrolyzing the etherized compound in the presence of an acid catalyst to remove the protecting group. By the method, the trifluoromethyl-substituted 2-alkoxyacetoxyphenone derivative can be produced in a remarkably better yield than by conventional methods. COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：提供一种用于工业生产用作药物和农药的重要中间体的三氟甲基取代的2-烷氧基乙酰氧基苯甲酮衍生物的方法。解决方案：用于制备三氟甲基取代的2-烷氧基乙酰氧基苯甲酮衍生物的方法包括在亚烷基二醇的存在下用Br 2 SB溴化三氟甲基取代的苯乙酮，将得到的溴化缩醛进行取代反应与金属醇盐反应，然后在酸催化剂存在下水解该化合物以除去保护基团。通过该方法，三氟甲基取代的2-烷氧基乙酰氧基苯甲酮衍生物可以以比常规方法显着更好的产率制备。版权所有（C）2004，JPO

12. 发明专利

JP2004099480A Optically active 1-(fluoro, trifluoromethyl or trifluoromethoxy-substituted phenyl)alkylamine n-monoalkyl derivative and method for producing the same 有权
公开(公告)号：JP2004099480A
公开(公告)日：2004-04-02
申请号：JP2002261148
申请日：2002-09-06
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO , OTSUKA TAKASHI , UEDA KOJI
IPC分类号： C07C209/62 , A61K31/137 , C07B61/00 , C07C209/52 , C07C211/29 , C07C213/08 , C07C217/58
CPC分类号： C07C209/62 , C07B2200/07 , C07C211/29 , C07C217/58 , C07C249/02 , C07C251/24
摘要： PROBLEM TO BE SOLVED: To provide a new optically active 1-(fluoro, trifluoromethyl or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative used as an important intermediate for medicines and agrochemicals, and to provide a method for producing the same. SOLUTION: This method for producing the optically active 1-(fluoro, trifluoromethyl or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by formula [4] [R is F, trifluoromethyl or trifluoromethoxy; (n) is an integer of 1 to 5; R 1 and R 2 are each a 1 to 6C alkyl; * shows an asymmetric carbon] comprises reacting an optically active secondary amine represented by formula [1] (Me is methyl; Ar is phenyl or naphthyl) with an alkylating agent represented by formula [2] (X is a releasable group) in the presence of a base and then hydrolyzing the obtained optically active tertiary amine represented by formula [3]. COPYRIGHT: (C)2004,JPO

13. 发明专利

JP2004067637A Method for producing trifluoromethyl-substituted 2-alkoxyacetophenone derivative 审中-公开
公开(公告)号：JP2004067637A
公开(公告)日：2004-03-04
申请号：JP2002232698
申请日：2002-08-09
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO , OTSUKA TAKASHI , UEDA KOJI
IPC分类号： C07D317/16 , C07B61/00 , C07C43/315 , C07C45/42 , C07C45/59 , C07C49/84 , C07D317/22 , C07D319/06 , C07D321/06
摘要： PROBLEM TO BE SOLVED: To provide a method for the industrial production of a trifluoromethyl-substituted 2-alkoxyacetophenone derivative usable as an important intermediate for pharmaceuticals and agrochemicals.
SOLUTION: The trifluoromethyl-substituted 2-alkoxyacetophenone derivative is produced in remarkably improved yield by protecting the carbonyl group of a trifluoromethyl-substituted phenacyl halide with acetal group to convert the halide into acetal, converting the product into an ether by the substitution reaction with a metal alkoxide and hydrolyzing and deprotecting the ether in the presence of an acid catalyst.
COPYRIGHT: (C)2004,JPO

14. 发明专利

JP2002371028A Method for producing 3,3,3-trifluoro-2-hydroxypropionic acid derivative 有权
标题翻译： 3,3,3-三氟-2-羟基丙酸衍生物的制备方法
公开(公告)号：JP2002371028A
公开(公告)日：2002-12-26
申请号：JP2001180412
申请日：2001-06-14
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KANAI MASATOMI , YASUMOTO MANABU , KURIYAMA KATSU , HAYAMIZU TAKASHI , KUME KOJI , IMURA HIDEAKI
IPC分类号： C07C51/093 , C07B61/00 , C07C51/347 , C07C59/01 , C07C59/125
摘要： PROBLEM TO BE SOLVED: To provide a producing method capable of efficiently obtaining a 3,3,3-trifluoro-2-hydroxypropionic acid derivative which is an important intermediate for medicines and agrochemicals.
SOLUTION: 1,1,1-Trichloro-3,3,3-trifluoro-2-propanol derivative is reacted with a base in methanol to produce a 3,3,3-trifluoro-2-methoxypropionic acid derivative, which is further demethylated to efficiently produce a 3,3,3- trifluoro-2-hydroxypropionic acid derivative.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：提供能够有效地获得作为药物和农药的重要中间体的3,3,3-三氟-2-羟基丙酸衍生物的制备方法。溶液：将1,1,1-三氯-3,3,3-三氟-2-丙醇衍生物与甲醇中的碱反应生成3,3,3-三氟-2-甲氧基丙酸衍生物，进一步脱甲基化以有效地制备3,3,3-三氟-2-羟基丙酸衍生物。

15. 发明专利

JP2006083163A Method for producing optically active alfa-fluorocarboxylic ester derivative 有权
标题翻译：用于生产光学活性的ALFA-氟代羧酸酯衍生物的方法
公开(公告)号：JP2006083163A
公开(公告)日：2006-03-30
申请号：JP2005236405
申请日：2005-08-17
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , TSURUTA HIDEYUKI , OTSUKA TAKASHI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO , UEDA KOJI
IPC分类号： C07C67/307 , C07B53/00 , C07B55/00 , C07C29/147 , C07C31/38 , C07C69/63 , C07C69/65
摘要： PROBLEM TO BE SOLVED: To provide an industrial method for producing an optically active α-fluorocarboxylic ester derivative that is an important intermediate for medicines and optical material. SOLUTION: The optically active α-fluorocarboxylic ester derivative is produced by allowing an optically active α-hydroxycarboxylic ester derivative to react with trifluoromethane sulfonyl fluoride in the presence of an industrially inexpensive and general-purpose organic base, for example, triethylamine or the like. The resultant optically active α-fluorocarboxylic ester derivative is allowed to react with a hydride reducing agent to obtain an optically active 2-fluoroalcohol derivative. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：提供一种用于制备作为药物和光学材料的重要中间体的光学活性α-氟代羧酸酯衍生物的工业方法。解决方案：光学活性α-氟代羧酸酯衍生物是通过使光学活性的α-羟基羧酸酯衍生物在工业上便宜且通用的有机碱（例如三乙胺）存在下与三氟甲磺酰氟反应制备的类似。使得到的光学活性α-氟代羧酸酯衍生物与氢化物还原剂反应，得到光学活性的2-氟代醇衍生物。版权所有（C）2006，JPO＆NCIPI

16. 发明专利

JP2005047870A Method for producing 4,4,4-trifluoro-2,3-epoxybutanoic acid ester 有权
标题翻译： 4,4,4-三氟-2,3-环氧丁酸酯的制备方法
公开(公告)号：JP2005047870A
公开(公告)日：2005-02-24
申请号：JP2003283118
申请日：2003-07-30
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO , OTSUKA TAKASHI , UEDA KOJI
IPC分类号： C07D303/48 , C07B53/00 , C07C45/63 , C07C49/82 , C07D301/26 , C07D303/32
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing a 4,4,4-trifluoro-2,3-epoxybutanoic acid ester which is an important intermediate for a medicine and an agrochemical.
SOLUTION: 4,4,4-Trifluoro-3-hydroxy-1-aryl-1-butanone is converted to 4,4,4-trifluoro-3-hydroxy-2-halogeno-1-aryl-1-butanone by being reacted with a halogenation reagent. The compound is converted to 4,4,4-trifluoro-2,3-epoxy-1-aryl-1-butanone by being reacted with a base, and an aryl 4,4,4-trifluoro-2,3-epoxybutanoate is produced by reacting the resultant compound with an oxidizing agent. An alkyl 4,4,4-trifluoro-2,3-epoxybutanoate is produced by reacting the compound with a lower alcohol. By the method, the subject compound is obtained in a yield extremely superior to the one by a conventional method.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供工业上制备作为药物和农药的重要中间体的4,4,4-三氟-2,3-环氧丁酸酯的方法。解决方案：将4,4,4-三氟-3-羟基-1-芳基-1-丁酮转化为4,4,4-三氟-3-羟基-2-卤代-1-芳基-1-丁酮通过与卤化试剂反应。该化合物通过与碱反应而转化为4,4,4-三氟-2,3-环氧-1-芳基-1-丁酮，4,4,4-三氟-2,3-环氧丁烷基的芳基是通过使所得化合物与氧化剂反应而制备。通过使该化合物与低级醇反应制备4,4,4-三氟-2,3-环氧丁烷酸烷基酯。通过该方法，通过常规方法获得极高的收率的主题化合物。版权所有（C）2005，JPO＆NCIPI

17. 发明专利

JP2004018503A Method for producing 3, 3, 3- trifluoro-2-hydroxypropionic acid and its derivative 有权
公开(公告)号：JP2004018503A
公开(公告)日：2004-01-22
申请号：JP2002179554
申请日：2002-06-20
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO
IPC分类号： C07C29/159 , C07C31/38 , C07C51/093 , C07C51/295 , C07C51/353 , C07C59/115
CPC分类号： C07C51/295 , C07C59/115
摘要： PROBLEM TO BE SOLVED: To provide a new method for producing 3, 3, 3-trifluoro-2-hydroxypropionic acid and its derivative which are important intermediates of a medicine and liquid crystal.
SOLUTION: The 3, 3, 3-trifluoro-2-hydroxypropionic acid is obtained by bringing 1, 1-dihalogeno-3, 3, 3-trifluoroacetone in contact with a basic aqueous solution, and then this acid is reacted with a lower alcohol under an acidic condition and converted into a 3, 3, 3-trifluoro-2-hydroxy propionic acid ester, and then performing the reaction of the 3, 3, 3-trifluoro-2-hydroxy propionic ester with a hydride reducing agent to obtain 3, 3, 3-trifluoro-2-hydroxypropanol.
COPYRIGHT: (C)2004,JPO

18. 发明专利

JP2003335737A Optically active (r)-1-(4-trifluoromethylphenyl) ethylamine 审中-公开
标题翻译：光学活性（R）-1-（4-三氟甲基苯基）乙基胺
公开(公告)号：JP2003335737A
公开(公告)日：2003-11-28
申请号：JP2002146983
申请日：2002-05-21
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , YASUMOTO MANABU , KURIYAMA KATSU , KANAI MASATOMI , INOMIYA NORITO
IPC分类号： C07C209/88 , C07C211/27 , C07C211/29 , C07C251/24
CPC分类号： C07C251/24 , C07C211/29
摘要： PROBLEM TO BE SOLVED: To provide a new optically active (R)-1-(4-trifluoromethylphenyl) ethylamine useful as an important intermediate for medicines and agrochemicals.
SOLUTION: This optically active (R)-1-(4-trifluoromethylphenyl) ethylamine can be synthesized in a high optical purity and in a good yield by subjecting 4'-(trifluoromethyl)acetophenone and optically active (R)-1-phenylethylamine to a dehydrative condensation under an acidic condition, asymmetrically reducing the obtained optically active imine into the optically active secondary amine, deriving the secondary amine into its phthalate or benzene sulfonate which are the organic acid salts, recrystallizing and purifying the organic acid salt, hydrolyzing the purified organic acid salt to produce the optically active (R)-1-(4- trifluoromethylphenyl)ethylamine phthalate or benzene sulfonate as the organic acid salt, and then neutralizing the product.
COPYRIGHT: (C)2004,JPO
摘要翻译：要解决的问题：提供用作药物和农药的重要中间体的新的光学活性（R）-1-（4-三氟甲基苯基）乙胺。解决方案：该光学活性（R）-1-（4-三氟甲基苯基）乙胺可以通过使4' - （三氟甲基）苯乙酮和光学活性（R）-1 - 苯基乙胺在酸性条件下脱水缩合，将得到的光学活性亚胺不对称地还原成光学活性仲胺，将仲胺导入作为有机酸盐的邻苯二甲酸酯或苯磺酸盐，重结晶并纯化有机酸盐，水解纯化的有机酸盐，得到光学活性（R）-1-（4-三氟甲基苯基）乙胺邻苯二甲酸酯或苯磺酸盐作为有机酸盐，然后中和产物。版权所有（C）2004，JPO

19. 发明专利

JP2008037781A Method for producing a 2'-deoxy-2'-fluoro uridine 有权
标题翻译：生产2'-脱氧-2'-氟尿嘧啶的方法
公开(公告)号：JP2008037781A
公开(公告)日：2008-02-21
申请号：JP2006212750
申请日：2006-08-04
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , OTSUKA TAKASHI , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , INOMIYA NORITO , UEDA KOJI , TSURUTA HIDEYUKI , MOGI KAORI
IPC分类号： C07H19/067
CPC分类号： Y02P20/52
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing 2'-deoxy-2'-fluorouridine which is an important intermediate for pharmaceuticals. SOLUTION: The objective 2'-deoxy-2'-fluorouridine is obtained by reacting a 1-β-D-arabinofuranosyluracil derivative (3',5'-hydroxy-protected compound) with sulfuryl fluoride (SO 2 F 2 ) in the presence of an organic base to convert into a 3',5'-hydroxy-protected compound of 2'-deoxy-2'-fluorouridine and then acting a deprotecting agent. COPYRIGHT: (C)2008,JPO&INPIT

20. 发明专利

JP2006008534A Method for producing 4-fluoroproline derivative 有权
标题翻译：生产4-氟吡啶衍生物的方法
公开(公告)号：JP2006008534A
公开(公告)日：2006-01-12
申请号：JP2004184099
申请日：2004-06-22
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , KURIYAMA KATSU , SUDO KATSUHIDE , OTSUKA TAKASHI , YASUMOTO MANABU , INOMIYA NORITO , UEDA KOJI , TSURUTA HIDEYUKI
IPC分类号： C07D207/16 , C07B53/00 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing a 4-fluoroproline derivative being an important intermediate for a medicine.
SOLUTION: The method for producing a 4-fluoroproline derivative comprises reacting a 4-hydroxyproline-protected compound with trifluoromethanesulfonyl fluoride in the presence of an organic base such as triethylamine, lutidine, collidine, etc., and (a salt or a complex composed of an organic base such as trimethylamine, pyridine, etc., and hydrogen fluoride). The first characteristic excellently advances dehydroxyfluorination reaction of a 4-hydroxyproline-protected compound by using trifluoromethanesulfonyl fluoride as a perfluoroalkanesulfonyl fluoride. The second characteristic excellently advances the dehydroxyfluorination reaction even in the presence of a fluorinating agent such as triethylamine-hydrogen trifluoride complex or (a salt or a complex composed of an organic base such as pyridine, etc., and hydrogen fluoride) except diisopropylethylamine-hydrogen trifluoride complex.
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供一种工业生产作为药物的重要中间体的4-氟脯氨酸衍生物的方法。解决方案：4-氟脯氨酸衍生物的制备方法包括在有机碱如三乙胺，二甲基吡啶，可力丁等存在下使4-羟基脯氨酸保护的化合物与三氟甲磺酰氟反应，和（盐或由有机碱如三甲胺，吡啶等组成的络合物和氟化氢）。第一个特征通过使用三氟甲磺酰氟作为全氟烷基磺酰氟，显着地提高了4-羟基脯氨酸保护的化合物的脱羟基氟化反应。第二个特征即使在氟化剂如三乙胺 - 三氟化氢络合物存在下也可以进行脱羟基氟化反应，或者除了二异丙基乙胺 - 氢以外（或由吡啶等有机碱组成的络合物和氟化氢）三氟化合物。版权所有（C）2006，JPO＆NCIPI

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