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1. 发明专利

JP2008013519A Production method for optically active 2-fluoroalcohol derivative 审中-公开
标题翻译：用于光活性2-氟代醇衍生物的生产方法
公开(公告)号：JP2008013519A
公开(公告)日：2008-01-24
申请号：JP2006188304
申请日：2006-07-07
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 , MOGI KAORI
IPC分类号： C07C29/147 , C07B55/00 , C07C31/38
摘要： PROBLEM TO BE SOLVED: To provide a production method suitable for producing an optically active 2-fluoroalcohol derivative on a large scale, which is an important intermediate of medicine and optical materials. SOLUTION: The optically active 2-fluoroalcohol derivative is produced by reacting an optically active α-hydroxycarboxylic ester derivative with sulfuryl fluoride in the presence of an organic base or in the presence of an organic base and "a salt or complex comprising an organic base and hydrogen fluoride" and then reacting the resultant optically active α-fluorocarboxylic ester derivative with a hydride reducing agent. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供适合于大规模生产光学活性的2-氟代醇衍生物的制备方法，其是药物和光学材料的重要中间体。解决方案：光学活性2-氟代醇衍生物通过光学活性的α-羟基羧酸酯衍生物与硫酰氟在有机碱的存在下或在有机碱的存在下反应而制备，“盐或络合物包含有机碱和氟化氢“，然后使所得光学活性α-氟代羧酸酯衍生物与氢化物还原剂反应。版权所有（C）2008，JPO＆INPIT

2. 发明专利

JP2005035961A Method for producing optically active 1-(2-trifluoromethylphenyl)ethylamine 有权
标题翻译：生产光学活性1-（2-三氟甲基苯基）乙基胺的方法
公开(公告)号：JP2005035961A
公开(公告)日：2005-02-10
申请号：JP2003277105
申请日：2003-07-18
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： C07C209/16 , C07B57/00 , C07C209/88 , C07C211/29 , C07C303/28 , C07C309/66
CPC分类号： C07C303/28 , C07B2200/07 , C07C211/29 , C07C309/66
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing optically active 1-(2-trifluoromethylphenyl)ethylamine which is an important intermediate for medicines and agrochemicals. SOLUTION: The method for producing optically active 1-(2-trifluoromethylphenyl)ethylamine or its salt comprises reacting 1-(2-trifluromethylphenyl)ethyl alcohol with a sulfonylating agent in the presence of a base to convert the compound to a sulfonate, reacting the sulfonate with optically active 1-phenylethylamine to produce a secondary amine, derivatizing the secondary amine to its salt, recrystallizing and refining its salt to refine the secondary amine into an optically active secondary amine and hydrolysing the optically active secondary amine or its salt. The production method provides the optically active 1-(2-trifluoromethylphenyl)ethylamine in remarkably better efficiency than conventional methods. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供工业上制造光学活性的1-（2-三氟甲基苯基）乙胺的方法，该方法是药物和农药的重要中间体。解决方案：光学活性1-（2-三氟甲基苯基）乙胺或其盐的制备方法包括在碱的存在下使1-（2-三氟甲基苯基）乙醇与磺酰化剂反应，将化合物转化成磺酸盐使磺酸盐与光学活性1-苯基乙胺反应以产生仲胺，将仲胺衍生为其盐，重结晶并精制其盐以将仲胺精制成光学活性仲胺并水解光学活性仲胺或其盐。该制备方法提供光学活性的1-（2-三氟甲基苯基）乙胺的显着效果比常规方法。版权所有（C）2005，JPO＆NCIPI

3. 发明专利

JP2004315434A Methods for producing trifluoromethyl-substituted 2-bromoacetophenone and trifluoromethyl-substituted 2-hydroxyacetophenone 审中-公开
公开(公告)号：JP2004315434A
公开(公告)日：2004-11-11
申请号：JP2003111930
申请日：2003-04-16
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , INOMIYA NORITO , KANAI MASATOMI , KURIYAMA KATSU , YASUMOTO MANABU , OTSUKA TAKASHI , UEDA KOJI
IPC分类号： C07C45/57 , C07B61/00 , C07C45/64 , C07C49/80 , C07C49/82
摘要： PROBLEM TO BE SOLVED: To provide methods for industrially producing trifluoromethyl-substituted 2-bromoacetophenone and trifluoromethyl-substituted 2-hydroxyacetophenone of important intermediates for a medicine and an agrochemical.
SOLUTION: The method for producing the trifluoromethyl-substituted 2-bromoacetophenone comprises brominating trifluoromethyl-substituted acetophenone with Br
2 in the presence of an alkylene diol so as to be converted to a cyclic acetal of the trifluoromethyl-substituted 2-bromoacetophenone, and reacting the cyclic acetal of the trifluoromethyl-substituted 2-bromoacetophenone with water under an acidic condition. The method for producing the trifluoromethyl-substituted 2-hydroxyacetophenone involves reacting the trifluoromethyl-substituted 2-bromoacetophenone with the water under an acidic or neutral condition. By the methods, the trifluoromethyl-substituted 2-bromoacetophenone and the trifluoromethyl-substituted 2-hydroxyacetophenone are obtained in an efficiency extremely superior to the one of a conventional method.
COPYRIGHT: (C)2005,JPO&NCIPI

4. 发明专利

JP2006022009A METHOD FOR PRODUCING 3-FLUORO-2,3-DIDEOXY-β-D-RIBOFURANOSYL-TYPE NUCLEOSIDE DERIVATIVE 审中-公开
标题翻译：生产3-氟-2,3-二脱氧-β-D-吡喃木糖型核苷衍生物的方法
公开(公告)号：JP2006022009A
公开(公告)日：2006-01-26
申请号：JP2004198851
申请日：2004-07-06
申请人： Ajinomoto Co Inc , Central Glass Co Ltd , セントラル硝子株式会社 , 味の素株式会社
发明人： ISHII AKIHISA , OTSUKA TAKASHI , KUME KOJI , KURIYAMA KATSU , TORII TAKAYOSHI , ONISHI TOMOYUKI , IZAWA KUNISUKE
IPC分类号： C07H1/00 , C07H19/16
CPC分类号： Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a 3-fluoro-2,3-dideoxy-β-D-ribofuranosyl-type nucleoside derivative, capable of industrially producing the derivative, especially 3'-fluoro-2',3'-dideoxyguanosine, at a low cost. SOLUTION: This 3-fluoro-2,3-dideoxy-β-D-ribofuranosyl-type nucleoside derivative is produced by reacting a 3-halogeno-3-dideoxy-β-D-xylofuranosyl-type nucleoside derivative with sulfur tetrafluoride (SF 4 ), so as to convert the xylofuranosyl-type derivative into a 2-halogeno-2,3-dideoxy-3-fluoro-β-D-arabinofuranosyl-type nucleoside derivative with high regioselectivity, and then conducting, irrespective of order, a process (1) for subjecting a halogen atom at the 2'-position to dehalogenation, a process (2) for subjecting a protective group for a hydroxy group at the 5'-position to deprotection, and, if necessary, a process (3) for conducting at least any one of protection, deprotection, and modification of a nucleic-acid base or its derivative. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供一种能够在工业上生产该衍生物的3-氟-2,3-二脱氧-β-D-呋喃核糖型核苷衍生物的制备方法，特别是3'-氟-2' ，3'-二脱氧鸟苷，成本低廉。解决方案：3-氟-2,3-二脱氧-β-D-呋喃核糖基型核苷衍生物通过3-卤代-3-二脱氧-β-D-木糖呋喃糖基型核苷衍生物与四氟化硫（SF 4 ），将该恶二糖基型衍生物转化为具有高区域选择性的2-卤代-2,3-二脱氧-3-氟-β-D-阿拉伯呋喃糖基型核苷衍生物，然后进行将2位的卤原子进行脱卤的步骤（1），不管其顺序如何，将在5'-位保护基进行羟基保护基脱保护的方法（2）如果需要，可以进行核酸碱基或其衍生物的保护，脱保护和修饰中的至少任一种的方法（3）。版权所有（C）2006，JPO＆NCIPI

5. 发明专利

JP2005247785A Optically active 1-aryl-2-fluoro-substituted ethylamine and method for producing the same 有权
标题翻译：光活性1-芳基-2-氟取代的乙酰胺及其生产方法
公开(公告)号：JP2005247785A
公开(公告)日：2005-09-15
申请号：JP2004062735
申请日：2004-03-05
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 , SUDO KATSUHIDE , UEDA KOJI
IPC分类号： C07C209/26 , C07B61/00 , C07C209/52 , C07C209/60 , C07C209/62 , C07C211/29 , C07C249/02 , C07C251/24
CPC分类号： C07C251/24 , C07C209/52 , C07C209/62 , C07C211/29 , C07C249/02
摘要： PROBLEM TO BE SOLVED: To provide an optically active 1-aryl-2-fluoro-substituted ethylamine becoming an important intermediate of a candidate compound of a medicine and an agrochemical, and an industrial method for producing the same. SOLUTION: This method for producing optically active 1-aryl-2-fluoro-substituted ethylamine is provided by performing the dehydrating condensation of a fluoro-substituted methyl aryl ketone with an optically active 1-phenylethylamine in the presence of an acid catalyst to convert them to an optically active imine, further asymmetrically reducing the optically active imine to convert it to a mixture of optically active secondary amine diastereomers, inducing the diastereomer mixture of the optically active secondary amines to their salts and recrystallizing to obtain the optically active secondary amine having a high diastereomeric excess rate or its salt, and hydrolyzing the optically active secondary amine or its salt in the presence of a group VIII transition metal catalyst to obtain the optically active 1-aryl-2-fluoro-substituted ethylamine or its salt. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供一种光学活性的1-芳基-2-氟取代的乙胺，成为药物和农药的候选化合物的重要中间体及其制备方法。解决方案：通过在酸催化剂的存在下进行氟取代的甲基芳基酮与光学活性1-苯基乙胺的脱水缩合来提供该光学活性1-芳基-2-氟取代的乙胺的制备方法将其转化为光学活性亚胺，进一步不对称地还原光学活性亚胺以将其转化为光学活性仲胺非对映体的混合物，将光学活性仲胺的非对映异构体混合物引入其盐并重结晶以获得光学活性二级胺，其具有高非对映体过量速率或其盐，并在VIII族过渡金属催化剂存在下水解光学活性仲胺或其盐以获得光学活性1-芳基-2-氟取代的乙胺或其盐。版权所有（C）2005，JPO＆NCIPI

6. 发明专利

JP2005213149A Method for producing trifluoromethyl-substituted acetophenone 审中-公开
标题翻译：生产三氟甲磺酸取代的乙酰丙酮的方法
公开(公告)号：JP2005213149A
公开(公告)日：2005-08-11
申请号：JP2004018316
申请日：2004-01-27
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , INOMIYA NORITO , UEDA KOJI , YASUMOTO MANABU , KANAI MASATOMI , KURIYAMA KATSU , OTSUKA TAKASHI , SUDO KATSUHIDE
IPC分类号： C07C45/30 , C07C49/80
摘要： PROBLEM TO BE SOLVED: To provide an industrial method for producing a trifluoromethyl-substituted acetophenone which is an important intermediate for medicines and agrochemicals.
SOLUTION: The method for producing the trifluoromethyl-substituted acetophenone is carried out by oxidizing a 1-trifluoromethyl-substituted phenylethanol with an aqueous solution of sodium hypochlorite at ≥10% available chlorine concentration in the presence of acetic acid in an amount of ≤20 equivalents based on the 1-trifluoromethyl-substituted phenylethanol. The method for production is remarkably improved in productivity and operation efficiency and is a more inexpensive method for production. The selectivity of the reaction is ultrahigh and impurities difficult to separate are scarcely formed as a by-product. Thereby, the method is extremely effective for industrial production in high purity.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供一种三氯甲基取代的苯乙酮的生产方法，其是药物和农药的重要中间体。解决方案：制备三氟甲基取代的苯乙酮的方法是通过在乙酸存在下以≥10％有效氯浓度的次氯酸钠水溶液氧化1-三氟甲基取代的苯基乙醇，其量为基于1-三氟甲基取代的苯乙醇，≤20当量。生产率和运行效率显着地提高了生产方法，并且是更廉价的生产方法。反应的选择性超高，难以分离的杂质几乎不作为副产物形成。因此，该方法对于高纯度的工业生产是非常有效的。版权所有（C）2005，JPO＆NCIPI

7. 发明专利

JP2004323518A Method for producing 2'-deoxy-2'-fluorouridine 有权
公开(公告)号：JP2004323518A
公开(公告)日：2004-11-18
申请号：JP2004115270
申请日：2004-04-09
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
IPC分类号： C07H19/06 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing 2'-deoxy-2'-fluorouridine which is an important intermediate for a pharmaceutical. SOLUTION: This method for producing the 2'-deoxy-2'-fluorouridine comprising reacting a 3',5'-hydroxy-protected compound of 1-β-D-arabinofuranosyluracil with a trifluoromethanesulfonylating agent in the presence of an organic base to convert the compound into a 2'-triflate compound thereof, then reacting the triflate compound with a fluorinating agent which comprises "a salt or a complex composed of an organic base and hydrofluoric acid" to produce a 3',5'-hydroxy-protected compound of the 2'-deoxy-2'-fluorouridine, and further acting a deprotecting agent on the produced compound. The obtained 2'-deoxy-2'-fluorouridine is once converted into a 3',5'-diacetyl compound thereof, and the 3',5'-diacetyl compound is deacetylated after it is recrystallized, so that the 2'-deoxy-2'-fluorouridine is efficiently purified to have high purity. COPYRIGHT: (C)2005,JPO&NCIPI

8. 发明专利

JP2004143087A Method for producing optically active 2-alkoxy-1-(trifluoromethyl-substituted phenyl)ethanol derivative 审中-公开
标题翻译：生产光学活性的2-烷氧基-1-（三氟甲基取代的苯基）乙醇衍生物的方法
公开(公告)号：JP2004143087A
公开(公告)日：2004-05-20
申请号：JP2002310180
申请日：2002-10-24
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： C07B53/00 , C07B61/00 , C07C41/26 , C07C43/178 , C07C59/56 , C07C67/08 , C07C69/732 , C07D309/12
CPC分类号： C07D309/12 , C07B2200/07 , C07C43/1786 , C07C59/56 , C07C69/732
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing an optically active 2-alkoxy-1-(trifluoromethyl-substituted phenyl)ethanol derivative in a high optical purity in a high yield which is an important intermediate for medicines and agrochemicals by using industrially readily obtainable starting raw materials.
SOLUTION: The method for producing the optically active 2-alkoxy-1-(trifluoromethyl-substituted phenyl)ethanol derivative in a high optical purity in a high yield comprises reacting optically active trifluoromethyl-substituted mandelic acid with a lower alcohol in the presence of an acid catalyst into an optically active trifluoromethyl-substituted mandelic acid ester, protecting the hydroxy group of the mandelic acid ester, reducing the resultant substance with a hydride reducing agent, reacting the obtained product with an alkylating agent in the presence of a base into the hydroxy group protected substance of an optically active 2-alkoxy-1-(trifluoromethyl-substituted phenyl)ethanol and then deprotecting the resulting substance.
COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：以高产率提供高光学纯度的光学活性2-烷氧基-1-（三氟甲基取代的苯基）乙醇衍生物的方法，其为药物和农药的重要中间体通过使用工业上容易获得的起始原料。解决方案：以高产率制备高光学纯度的光学活性2-烷氧基-1-（三氟甲基取代的苯基）乙醇衍生物的方法包括使光学活性的三氟甲基取代的扁桃酸与低级醇在将酸催化剂存在于光学活性的三氟甲基取代的扁桃酸酯中，保护扁桃酸酯的羟基，用氢化物还原剂还原所得的物质，使得到的产物与烷基化剂在碱的存在下反应转化为光学活性2-烷氧基-1-（三氟甲基取代的苯基）乙醇的羟基保护物质，然后使得到的物质脱保护。版权所有（C）2004，JPO

9. 发明专利

JP2005336151A 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：JP2005336151A
公开(公告)日：2005-12-08
申请号：JP2004215526
申请日：2004-07-23
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
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially producing a 4-fluoroproline derivative which is an important intermediate for a pharmaceutical. SOLUTION: This method for producing the 4-fluoroproline derivative comprises making a protected 4-hydroxyproline compound react with trifluoromethanesulfonyl fluoride in the presence of an organic base, wherein an organic base which is industrially produced at a low cost and generally used, such as triethylamine, is used as the organic base. The method is characterized so that trifluoromethanesulfonylation of the protected 4-hydroxyproline compound is well progressed by using the trifluoromethanesulfonyl fluoride and subsequent fluorine substitution reaction is well progressed only by of a hydrofluoric acid salt or complex of the organic base, such as the trimethylamine, which is by-produced in an equivalent amount in a reaction system of the trifluoromethanesulfonylation. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供工业生产作为药物重要中间体的4-氟脯氨酸衍生物的方法。解决方案：制备4-氟脯氨酸衍生物的方法包括在有机碱的存在下使受保护的4-羟基脯氨酸化合物与三氟甲磺酰氟反应，其中以低成本和通常使用的工业生产的有机碱，例如三乙胺用作有机碱。该方法的特征在于，通过使用三氟甲磺酰氟，保护的4-羟基脯氨酸化合物的三氟甲磺酰化进行得很好，随后的氟取代反应仅通过氢氟酸盐或有机碱如三甲胺的络合物进行，其中在三氟甲磺酰化反应体系中以相当量副产。版权所有（C）2006，JPO＆NCIPI

10. 发明专利

JP2005002036A Method for preparing optically active 1-alkyl substituted-2,2,2-trifluoroethylamine 有权
标题翻译：制备光学活性1-烷基取代的2,2,2-三氟乙酰胺的方法
公开(公告)号：JP2005002036A
公开(公告)日：2005-01-06
申请号：JP2003166525
申请日：2003-06-11
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 , YASUMOTO MANABU , KANAI MASATOMI , INOMIYA NORITO , OTSUKA TAKASHI , UEDA KOJI
IPC分类号： C07C209/52 , C07B53/00 , C07B61/00 , C07C209/62 , C07C211/15 , C07C249/02 , C07C251/08
CPC分类号： C07C209/62 , C07B2200/07 , C07C209/52 , C07C211/15 , C07C249/02 , C07C251/08
摘要： PROBLEM TO BE SOLVED: To provide a method for industrially preparing an optically active 1-alkyl-substituted-2,2,2-trifluoroethylamine which is an important intermediate for a drug or an agricultural chemical.
SOLUTION: The method for preparing the optically active 1-alkyl-substituted-2,2,2-trifluoroethylamine or its salt comprises converting an optically active imine [an optically active N-(1-alkyl-2,2,2-trifluoroethylidene)-1-phenylethylamine] to an optically active secondary amine by asymmetric reduction in a hydrogen atmosphere with the use of a group VIII metal catalyst, leading the secondary amine to its salt, purifying the salt by recrystallization, and subjecting the secondary amine or the salt to hydrogenolysis. By this method, the optically active 1-alkyl-substituted-2,2,2-trifluoroethylamine can be obtained with far more efficiency than before.
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或农药的重要中间体的光学活性1-烷基取代-2,2,2-三氟乙胺的方法。解决方案：制备光学活性1-烷基取代-2,2,2-三氟乙胺或其盐的方法包括将光学活性亚胺[光学活性的N-（1-烷基-2,2,2 - 三氟亚乙基）-1-苯基乙胺]通过使用VIII族金属催化剂在氢气气氛中不对称还原而转化为光学活性仲胺，导致仲胺转化为其盐，通过重结晶纯化该盐，并使仲胺或盐进行氢解。通过该方法，可以以比以前更高的效率获得光学活性的1-烷基取代的-2,2,2-三氟乙胺。版权所有（C）2005，JPO＆NCIPI

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