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1. 发明专利

JP2010241770A Method for synthesizing isoindoline intermediate derivative 审中-公开
标题翻译：用于合成ISOINDOLINE中间体衍生物的方法
公开(公告)号：JP2010241770A
公开(公告)日：2010-10-28
申请号：JP2009095229
申请日：2009-04-09
申请人： Central Glass Co Ltd , Maruishi Pharmaceutical Co Ltd , セントラル硝子株式会社 , 丸石製薬株式会社
发明人： NISHIMURA MASAHITO , SUGAWARA NORIMITSU , NIGORIKAWA YASUKO , INOMIYA NORITO , UEDA KOJI , ISHII AKIHISA , KANEMITSU NORIAKI
IPC分类号： C07D209/70
摘要： PROBLEM TO BE SOLVED: To provide a total synthetic route of an isoindoline intermediate derivative and isoindoline final derivative, enabling the mass production of the isoindoline final derivative as the final compound industrially and economically.
SOLUTION: This method for synthesizing the isoindoline intermediate derivative expressed by formula (8) comprises reacting an indane dicarboxylic acid with a compound expressed by formula (a) [wherein, Ph is phenyl; and Bn is benzyl] and then further reacting with aniline.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供异二氢吲哚中间体衍生物和异吲哚啉最终衍生物的总合成路线，使得能够在工业上和经济上大量生产异吲哚啉最终衍生物作为最终化合物。解决方案：用于合成由式（8）表示的异二氢吲哚中间体衍生物的方法包括使茚满二羧酸与式（a）表示的化合物反应[其中，Ph为苯基; 并且Bn是苄基]，然后与苯胺进一步反应。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2010285365A Method of synthesizing intermediate derivative of isoindoline 审中-公开
标题翻译：合成ISOINDOLINE中间衍生物的方法
公开(公告)号：JP2010285365A
公开(公告)日：2010-12-24
申请号：JP2009139049
申请日：2009-06-10
申请人： Central Glass Co Ltd , Maruishi Pharmaceutical Co Ltd , セントラル硝子株式会社 , 丸石製薬株式会社
发明人： NISHIMURA MASAHITO , SUGAWARA NORIMITSU , NIGORIKAWA YASUKO , INOMIYA NORITO , ISHII AKIHISA , KANEMITSU NORIAKI
IPC分类号： C07D209/70 , B01J31/24 , C07B61/00 , C07C17/12 , C07C25/22 , C07C51/10 , C07C63/38
CPC分类号： Y02P20/52
摘要： PROBLEM TO BE SOLVED: To provide a complete route of synthesizing an intermediate derivative of isoindoline and a final derivative of isoindoline, which route enables industrial, economical and large scale production of the final derivative of isoindoline. SOLUTION: The method of producing an intermediate derivative of isoindoline represented by formula (10) includes, (1) allowing indandicarboxylic acid anhydride to react with a specific Wittig reagent, (2) allowing the reaction product to react with aniline to produce an isoindoline derivative, (3) catalytically hydrogenating the isoindoline derivative in the presence of an asymmetric catalyst, and (4) subjecting the ester segment of the reaction product to hydrolysis or hydrogenolysis. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供合成异二氢吲哚的中间体衍生物和异二氢吲哚的最终衍生物的完整途径，该途径使工业，经济和大规模生产异二氢吲哚的最终衍生物。解决方案：由式（10）表示的异吲哚啉的中间体衍生物的制备方法包括：（1）使茚满二羧酸酐与特定的维蒂希试剂反应，（2）使反应产物与苯胺反应生成异二氢吲哚衍生物，（3）在不对称催化剂存在下催化氢化异二氢吲哚衍生物，和（4）使反应产物的酯链段进行水解或氢解。版权所有（C）2011，JPO＆INPIT

3. 发明专利

JP2010229098A Method for producing type a crystal form of isoindoline derivative and type a crystal form of isoindoline derivative 审中-公开
标题翻译：生产ISOINDOLINE衍生物和A型晶体衍生物晶型的A型晶体形式的方法
公开(公告)号：JP2010229098A
公开(公告)日：2010-10-14
申请号：JP2009079593
申请日：2009-03-27
申请人： Central Glass Co Ltd , Maruishi Pharmaceutical Co Ltd , セントラル硝子株式会社 , 丸石製薬株式会社
发明人： NIGORIKAWA YASUKO , SUGAWARA NORIMITSU , NISHIMURA MASAHITO , ISHII AKIHISA , KANEMITSU NORIAKI
IPC分类号： C07D209/94 , A61K31/496 , A61P25/20
摘要： PROBLEM TO BE SOLVED: To provide a method for producing an isoindoline derivative having a fixed crystal form, especially a method for selectively producing type A crystal form of isoindoline derivative.
SOLUTION: The method for producing type A crystal of isoindoline derivative represented by formula (1) includes: (a) a step for dissolving a crude body of the isoindoline derivative in at least one organic solvent selected from the group consisting of a 1-4C alcohol, a 2-6C ketone and others, and preparing a solution containing the isoindoline derivative and (b) a step for recrystallizing type A crystal form of the isoindoline derivative from the solution in the presence of type A seed crystal of the isoindoline derivative.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供具有固定结晶形式的异二氢吲哚衍生物的制备方法，特别是选择性生产异二氢吲哚衍生物的A型结晶形式的方法。解决方案：由式（1）表示的异二氢吲哚衍生物的A型晶体的制造方法包括：（a）将异二氢吲哚衍生物的粗体溶解在至少一种选自以下的有机溶剂中的工序： 1-4C醇，2-6C酮等，制备含有异二氢吲哚衍生物的溶液，（b）在A型晶种的存在下，从溶液中重结晶A型晶型的异二氢吲哚衍生物的工序异二氢吲哚衍生物。版权所有（C）2011，JPO＆INPIT

4. 发明专利

JP2013180975A METHOD OF MANUFACTURING α,α-DIFLUORO AROMATIC COMPOUND 有权
标题翻译：制备α，α-DIFLORO芳族化合物的方法
公开(公告)号：JP2013180975A
公开(公告)日：2013-09-12
申请号：JP2012045360
申请日：2012-03-01
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , YAMAZAKI TAKAKO , NISHINOMIYA TAKAYUKI , WATANABE MINEO
IPC分类号： C07C17/087 , C07C17/21 , C07C22/08 , C07C25/13
摘要： PROBLEM TO BE SOLVED: To provide a method capable of manufacturing an α,α-difluoro aromatic compound (a CFgroup directly bonds to an aromatic ring) in which high yield cannot be expected, industrially at low cost, in good yield, without requiring a high toxic catalyst, with simple operation, and with the use of a simple reactor.SOLUTION: A method of manufacturing an α,α-difluoro aromatic compound includes a process to make 1-chloro-1-aromatic ring substitution ethenes react with " a salt or complex consisting of an organic base and hydrogen fluoride". 1-chloro-1-aromatic ring substitution ethenes and "the salt or complex consisting of an organic base and hydrogen fluoride" can be obtained at comparatively low cost and at a large-amount scale. Moreover, an adopted reaction condition is mild, thereby selectivity is high and yield is also excellent. Further, a high toxic catalyst is not needed, a reactor is simple, and operation is also convenient. The present invention is very useful in this manner as an industrial manufacturing method of the α,α-difluoro aromatic compound.
摘要翻译：要解决的问题：提供一种能够以低成本，低成本，高产率地制造能够高产率地得到高收率的α，α-二氟芳香族化合物（CF基直接键合到芳香环上）的方法，而不需要高毒性催化剂，操作简单，并且使用简单的反应器。解决方案：制备α，α-二氟芳族化合物的方法包括使1-氯-1-芳环取代乙烯与“a”反应的方法由有机碱和氟化氢组成的盐或络合物“。 1-氯-1-芳环取代乙烯和“由有机碱和氟化氢组成的盐或络合物”可以以相对较低的成本和大规模获得。此外，采用的反应条件温和，选择性高，产率也优异。此外，不需要高毒性催化剂，反应器简单，操作也方便。本发明作为α，α-二氟芳香族化合物的工业制造方法是非常有用的。

5. 发明专利

JP2013028569A Method of producing geminal difluoro compound 审中-公开
标题翻译：生产金属歧化物化合物的方法
公开(公告)号：JP2013028569A
公开(公告)日：2013-02-07
申请号：JP2011166797
申请日：2011-07-29
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , YAMAZAKI TAKAKO
IPC分类号： C07C17/093 , C07B61/00 , C07C19/08 , C07C23/10 , C07C69/75
CPC分类号： C07C17/093 , C07C17/361 , C07C67/307 , C07C303/24 , C07C303/30 , C07C2601/14 , C07C69/75 , C07C305/26 , C07C309/65 , C07C23/10 , C07C19/08
摘要： PROBLEM TO BE SOLVED: To provide a method of producing a germinal difluoro compound, by which a raw material substrate is easily available, operations are easy and a high yield is obtained.SOLUTION: The method of producing the geminal difluoro compound includes a step of reacting fluorine-containing sulfuric acid enol esters with a fluorinating agent (hydrogen fluoride, "a salt or a complex comprising an organic base and hydrogen fluoride" or the like). The method is extremely useful for the production of the geminal difluoro compound, which solves all the problems in the prior arts.
摘要翻译：要解决的问题：为了提供生产二氟化合物的方法，通过该方法可以容易地获得原料基材，操作容易并且获得高产率。解决方案：制备偕二氟化合物的方法包括使含氟硫酸烯醇酯与氟化剂（氟化氢，“盐或包含有机碱和氟化氢的络合物”等）反应的步骤）。该方法对于生产偕二氟化合物是非常有用的，其解决了现有技术中的所有问题。版权所有（C）2013，JPO＆INPIT

6. 发明专利

JP2012162517A Method for producing fluoroamines 有权
标题翻译：生产氟菊酯的方法
公开(公告)号：JP2012162517A
公开(公告)日：2012-08-30
申请号：JP2012003742
申请日：2012-01-12
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 , NAGURA HIROKATSU , NIGORIKAWA YASUKO
IPC分类号： C07C303/40 , C07C209/62 , C07C211/08 , C07C311/16
CPC分类号： C07C303/38 , C07C209/62 , C07C303/40 , Y02P20/55 , C07C311/17 , C07C311/16 , C07C211/15
摘要： PROBLEM TO BE SOLVED: To provide a useful method for producing fluoroamines.SOLUTION: Fluoroamines can be produced by: protecting an amino group of an amino alcohol with a nitrobenzenesulfonyl group, thereby converting into a protected amino alcohol (amino group protection step); causing the protected amino alcohols to react with sulfuryl fluoride (SOF) in the presence of an organic base, thereby converting into a protected fluoroamine (dehydroxyfluorination step); and eliminating the protective group of the amino group of the protected fluoroamines (deprotection step). Since a nitrobenzenesulfonyl group highly satisfies the conditions required for the protective group of an amino group, an aimed fluoroamine can be obtained with high purity and high yield.
摘要翻译：待解决的问题：提供生产氟胺的有用方法。解决方案：氟胺可以通过：用硝基苯磺酰基保护氨基醇的氨基，从而转化成保护的氨基醇（氨基保护步骤）; 使有保护的氨基醇在有机碱的存在下与硫酰氟反应（SO 3 SB POS =“POST”> 2 ），由此转化保护的氟胺（脱羟基氟化步骤）; 并除去保护的氟胺的氨基的保护基（脱保护步骤）。由于硝基苯磺酰基高度满足氨基保护基所需的条件，因此可以获得高纯度和高收率的目标氟代胺。版权所有（C）2012，JPO＆INPIT

7. 发明专利

JP2012144511A METHOD FOR PRODUCING (2R)-2-FLUORO-2-C-METHYL-D-RIBONO-γ-LACTONE PRECURSOR 有权
标题翻译：（2R）-2-氟-2-C-甲基-D-糠基-γ-乳酸酯前体的制备方法
公开(公告)号：JP2012144511A
公开(公告)日：2012-08-02
申请号：JP2011082364
申请日：2011-04-04
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , NAGURA HIROKATSU , TSURUTA HIDEYUKI
IPC分类号： C07C67/327 , C07C69/24 , C07D307/33 , C07D317/30
CPC分类号： C07D317/30 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide an industrial method for producing (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor.SOLUTION: The open-ring fluorinated compound of the (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor can be produced by reacting 1, 2 diols with an organic base, and further with sulfuryl fluoride (SOF) in the presence of a fluoride ion source, as necessary. The method for producing the (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor invloves the fewer number of steps compared to the conventional production method (three steps consisting of cyclic sulfite esterification and oxidizing and ring-opening fluoridizing can be reduced to one step) and, further, fulfills the requisites (high yield and excellent reproducibility) as the industrial production method. The (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor thus obtained can be used as the important intermediate of 2'-deoxy-2'-fluoro-2'-C-methylcytidine having anti-viral activity.
摘要翻译：待解决的问题：提供（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体的工业方法。解决方案：（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体的开环氟化合物可以通过使1,2-二醇与有机碱反应制备，和根据需要，在氟化物离子源的存在下，进一步加入硫酰氟（SO 3 SB POS =“POST”> 2 ）。（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体的制备方法与常规的制备方法相比，步骤数量减少（由环状亚硫酸酯化和氧化和开环氟化可以减少到一个步骤），并且进一步满足工业生产方法的要求（高产率和优异的再现性）。所得到的（2R）-2-氟-2-C-甲基-D-内罗糖-γ-内酯前体可用作2'-脱氧-2'-氟-2'-C-甲基胞苷的重要中间体，其具有抗病毒活性。版权所有（C）2012，JPO＆INPIT

8. 发明专利

JP2012067037A METHOD OF PRODUCING α,α-DIFLUORO ESTERS 有权
标题翻译：生产α，α-不饱和酯的方法
公开(公告)号：JP2012067037A
公开(公告)日：2012-04-05
申请号：JP2010213545
申请日：2010-09-24
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , YAMAZAKI TAKAKO , TSURUTA HIDEYUKI , ISHIMARU TAKEHISA , NISHINOMIYA TAKAYUKI
IPC分类号： C07C67/307 , C07C69/63
摘要： PROBLEM TO BE SOLVED: To provide a practical method of producing α,α-difluoro esters important as pharmaceutical and agricultural chemical intermediates.SOLUTION: The α,α-difluoro esters are produced by reacting α-halogeno-α-fluoro esters with salts or complexes comprising an organic base and hydrogen fluoride. Dehydrohalogenation of side reaction is controlled in the production method. Only α-fluoro-α,β-unsaturated esters of by-products are treated to be brought specifically into a high boiling-point, a boiling point difference gets remarkably large thereby between the α,α-difluoro ester of an objective product and the unsaturated ester of by-product, and a high purity product of the objective product is efficiently obtained by fractional distillation of a simple operation. The method is the practical method of producing the α,α-difluoro esters capable of solving a problem point in a prior technique.
摘要翻译：待解决的问题：提供生产作为药物和农业化学中间体重要的α，α-二氟酯的实用方法。解决方案：α，α-二氟酯通过α-卤代-α-氟酯与包含有机碱和氟化氢的盐或络合物反应来制备。在生产方法中控制副反应的脱卤化氢。只有副产物的α-氟-α，β-不饱和酯被特别处理成高沸点，沸点差异显着，因此目标产物的α，α-二氟酯与副产物的不饱和酯和目标产物的高纯度产物通过简单操作的分馏而有效地获得。该方法是生产能够解决现有技术中的问题点的α，α-二氟酯的实用方法。版权所有（C）2012，JPO＆INPIT

9. 发明专利

JP2011231071A Optical resolution which obtains optical activity (r)-1-(4-fluoro phenyl)ethylamine 有权
标题翻译：获得光活性（R）-1-（4-氟代苯基）乙基胺的光学解决方案
公开(公告)号：JP2011231071A
公开(公告)日：2011-11-17
申请号：JP2010104451
申请日：2010-04-28
申请人： Central Glass Co Ltd , セントラル硝子株式会社
发明人： ISHII AKIHISA , UEDA KOJI , KATO MISUGI , YASUMOTO MANABU , OTSUKA TAKASHI , TSURUTA HIDEYUKI
IPC分类号： C07C209/88 , C07B57/00 , C07C59/245 , C07C211/29
摘要： PROBLEM TO BE SOLVED: To provide an industrial optical resolution which obtains optical activity (R)-1-(4-fluoro phenyl)ethylamine.SOLUTION: The optical resolution is carried out using natural type L-(-)-malic acid as a resolving agent, thereby optical activity (R)-1-(4-fluoro phenyl)ethylamine can be obtained. Further, the optical resolution is combined with an optical resolution which uses natural type L-(+)-tartaric acid for a resolving agent to obtain optical activity (S)-1-(4-fluoro phenyl)ethylamine, thereby a resolution efficiency of optical activity (R)-1-(4-fluoro phenyl)ethylamine can be improved. Moreover, in the optical resolution, a salt which consists of optical activity (R)-1-(4-fluoro phenyl)ethylamine and natural type L-(-)-malic acid and becomes a key diastereomer salt has been found out as a novel compound.
摘要翻译：要解决的问题：提供获得光学活性（R）-1-（4-氟苯基）乙胺的工业光学分辨率。解决方案：使用天然型L - （ - ） - 苹果酸作为拆分剂进行光学拆分，由此可以得到光学活性（R）-1-（4-氟苯基）乙胺。此外，光学分辨率与使用天然型L - （+） - 酒石酸用于拆分剂以获得光学活性（S）-1-（4-氟苯基）乙胺的光学拆分相结合，从而分辨率为可以改善光学活性（R）-1-（4-氟苯基）乙胺。此外，在光学拆分中，已经发现由光活性（R）-1-（4-氟苯基）乙胺和天然型L - （ - ） - 苹果酸组成并成为关键非对映异构体盐的盐作为新化合物。版权所有（C）2012，JPO＆INPIT

10. 发明专利

JP2010116331A METHOD FOR PRODUCING α-SUBSTITUTED ESTERS 有权
标题翻译：生产α-替代酯的方法
公开(公告)号：JP2010116331A
公开(公告)日：2010-05-27
申请号：JP2008289205
申请日：2008-11-11
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
IPC分类号： C07C67/30 , C07B53/00 , C07B61/00 , C07C69/612
CPC分类号： C07B53/00 , C07B55/00 , C07B2200/07 , C07C67/343 , C07C303/24 , C07C69/612 , C07C305/26
摘要： PROBLEM TO BE SOLVED: To provide a practical method for providing an α-substituted ester. SOLUTION: The α-substituted ester is produced by reacting a fluorosulfuric acid ester of α-hydroxy ester with a Grignard reagent in the presence of a zinc catalyst. Conventionally, a reaction in which a raw material substrate is limited to expensive trifluoromethanesulfonic acid is newly found to progress even in a fluorosulfuric acid ester suitable for production on a large amount scale. The α-substituted ester having inverted stereochemistry is obtained in a high optical purity by using the fluorosulfuric acid ester having high optical purity. The production method solves the whole problems of conventional technology and is industrially performed. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供一种提供α-取代酯的实用方法。解决方案：α-取代的酯通过在锌催化剂存在下使α-羟基酯的氟代硫酸酯与格氏试剂反应来制备。通常，即使在适合大规模生产的氟硫酸酯中，新发现原料基板被限制为昂贵的三氟甲磺酸的反应。通过使用具有高光学纯度的氟硫酸酯，以高光学纯度获得具有反相立体化学的α-取代酯。该生产方法解决了传统技术的全部问题，并在工业上得到了应用。版权所有（C）2010，JPO＆INPIT

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