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21. 发明申请

US20110213176A1 Process for Producing alpha Substituted Ester 有权
标题翻译：生产α取代酯的方法
公开(公告)号：US20110213176A1
公开(公告)日：2011-09-01
申请号：US13127955
申请日：2009-10-22
申请人： Akihiro Ishii , Manabu Yasumoto
发明人： Akihiro Ishii , Manabu Yasumoto
IPC分类号： C07C67/343
CPC分类号： C07B53/00 , C07B55/00 , C07B2200/07 , C07C67/343 , C07C303/24 , C07C69/612 , C07C305/26
摘要： There is provided a process for producing an α-substituted ester by reaction of a fluorosulfuric acid ester of α-hydroxyester with a Grignard reagent in the presence of a zinc catalyst. It is newly found that the reaction for production of α-substituted esters, in which the raw reaction substrate is limited to expensive trifluoromethanesulfonic acid esters, can proceed favorably with the use of fluorosulfuric acid esters suitable for mass-production uses. By the use of the fluorosulfuric acid ester high in optical purity, it is possible to obtain the α-substituted ester with high optical purity upon inversion of the asymmetric carbon configuration. The process of the present invention can solve all of the prior art problems and can be applied for industrial uses.
摘要翻译：提供了在锌催化剂存在下，通过α-羟基酯的氟代硫酸酯与格氏试剂的反应制备α-取代的酯的方法。新发现，通过使用适合于批量生产用途的氟代硫酸酯，可以有利地进行生产反应底物被限制为昂贵的三氟甲磺酸酯的α-取代酯的反应。通过使用光学纯度高的氟代硫酸酯，可以通过不对称碳结构的反转获得具有高光学纯度的α-取代的酯。本发明的方法可以解决所有现有技术的问题，并且可以应用于工业用途。

22. 发明授权

US07186865B2 Optically active 1-(fluoro-, trifluoromethyl-or trifluoromethoxy-substituted phenyl) alkylamine n-monoalkyl derivatives and process for producing same 有权
标题翻译：光学活性1-（氟 - ，三氟甲基 - 或三氟甲氧基取代的苯基）烷基胺n-单烷基衍生物及其制备方法
公开(公告)号：US07186865B2
公开(公告)日：2007-03-06
申请号：US10476650
申请日：2003-09-05
申请人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
发明人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
IPC分类号： C07C211/00
CPC分类号： C07C209/62 , C07B2200/07 , C07C211/29 , C07C217/58 , C07C249/02 , C07C251/24
摘要： An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4 is produced by a process including (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent R2—X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, each of R1 and R2 independently represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, * represents a chiral carbon, and X represents a leaving group.
摘要翻译：由式4表示的光学活性1-（氟 - ，三氟甲基 - 或三氟甲氧基取代的苯基）烷基胺N-单烷基衍生物通过以下方法制备，该方法包括：（a）使由式1表示的光学活性仲胺与式烷基化剂R 2 -X在碱的存在下，由此将仲胺转化成由式3表示的光学活性叔胺; 和（b）使叔胺进行氢解，从而制备N-单烷基衍生物，其中R表示氟原子，三氟甲基或三氟甲氧基，n表示1〜5的整数，R 1 独立地表示碳原子数1〜6的烷基，Me表示甲基，Ar表示苯基或1-或2-萘基， *表示手性碳，X表示离去基团。

23. 发明申请

US20060247433A1 Process for producing 2'-deoxy-2'-fluorouridine 失效
标题翻译：制备2'-脱氧-2'-氟尿苷的方法
公开(公告)号：US20060247433A1
公开(公告)日：2006-11-02
申请号：US10552463
申请日：2004-04-09
申请人： Akihiro Ishii , Takashi Ootsuka , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Koji Ueda
发明人： Akihiro Ishii , Takashi Ootsuka , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Koji Ueda
IPC分类号： C07H19/12
CPC分类号： C07H19/067 , Y02P20/55
摘要： 1-β-D-Arabinofuranosyluracil in 3′,5′-hydroxyl-protected form is reacted with a trifluoromethanesulfonylating agent in the presence of an organic base to convert it into a 2′-triflate form, and then it is reacted with a fluorinating agent containing “a salt or complex formed by an organic base and hydrofluoric acid” to produce 2′-deoxy-2′-fluorouridine in 3′,5′-hydroxyl-protected form. A deprotecting agent is further caused to act thereon to obtain 2′-deoxy-2′-fluorouridine. The 2′-deoxy-2′-fluorouridine obtained can efficiently be purified by temporarily converting it into a 3′,5′-diacetyl form, recrystallizing the 3′,5′-diacetyl form, and then deacetylating it. Thus, high-purity 2′-deoxy-2′-fluorouridine can be produced.
摘要翻译： 3'，5'-羟基保护形式的1-β-D-阿拉伯呋喃糖尿嘧啶在有机碱的存在下与三氟甲磺酰化剂反应，将其转化为2,3-三氟甲磺酸酯形式，然后与氟化含有“由有机碱和氢氟酸形成的盐或络合物”的试剂以产生3'，5'-羟基保护形式的2'-脱氧-2'-氟尿苷。进一步使脱保护剂作用于其上，得到2'-脱氧-2'-氟尿苷。所得到的2'-脱氧-2'-氟尿苷可以通过暂时转化为3'，5'-二乙酰基形式，重结晶3'，5'-二乙酰基形式，然后脱乙酰化而有效地纯化。因此，可以制备高纯度2'-脱氧-2'-氟尿苷。

24. 发明申请

US20060128976A1 Process for producing trifluoromethyl-substituted 2-alkoxyacetophenone derivatives 失效
标题翻译：制备三氟甲基取代的2-烷氧基苯乙酮衍生物的方法
公开(公告)号：US20060128976A1
公开(公告)日：2006-06-15
申请号：US11347390
申请日：2006-02-06
申请人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
发明人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
IPC分类号： C07D317/00 , C07D309/00
CPC分类号： C07D317/22 , C07C43/315 , C07C45/57 , C07C45/59 , C07C45/60 , C07C49/84 , C07D317/16 , C07C49/80
摘要： A process for producing a brominated acetal (represented by the formula 3) includes (a) brominating a trifluoromethyl-substituted acetophenone by Br2 in the presence of an alkylene diol. It is optional to produce a trifluoromethyl-substituted 2-alkoxyacetophenone derivative (represented by the formula 9) by (b) reacting the brominated acetal with a metal alkoxide, thereby converting the brominated acetal into an ether; and (c) hydrolyzing the ether in the presence of an acid catalyst to remove an acetal group from the ether, thereby producing the 2-alkoxyacetophenone derivative. Alternatively, the 2-alkoxyacetophenone can be produced by (a) reacting a trifluoromethyl-substituted phenacyl halide with an acetalization agent, thereby converting the phenacyl halide into an acetal; (b) reacting the acetal with a metal alkoxide, thereby converting the acetal into an ether; and (c) hydrolyzing the ether in the presence of an acid catalyst to remove the acetal group from the ether.
摘要翻译：制备溴化缩醛的方法（由式3表示）包括（a）在亚烷基二醇的存在下用Br 2 H 3溴化三氟甲基取代的苯乙酮。（b）使溴化缩醛与金属醇盐反应，从而将溴化缩醛转化成醚，任选地制备三氟甲基取代的2-烷氧基苯乙酮衍生物（由式9表示）和（c）在酸催化剂的存在下水解醚，以从乙醚中除去缩醛基，从而制备2-烷氧基苯乙酮衍生物。或者，2-烷氧基苯乙酮可以通过以下方法制备：（a）使三氟甲基取代的苯甲酰甲基卤化物与缩醛化剂反应，从而将苯甲酰甲酰卤转化成缩醛; （b）使缩醛与金属醇盐反应，从而将缩醛转化成醚; 和（c）在酸催化剂存在下水解该醚，以从乙醚中除去缩醛基。

25. 发明授权

US07053248B2 Process for producing trifluoromethyl- substituted 2- alkoxyacetophenone derivatives 有权
标题翻译：制备三氟甲基取代的2-烷氧基苯乙酮衍生物的方法
公开(公告)号：US07053248B2
公开(公告)日：2006-05-30
申请号：US10473399
申请日：2003-08-08
申请人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
发明人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
IPC分类号： C07C45/61
CPC分类号： C07D317/22 , C07C43/315 , C07C45/57 , C07C45/59 , C07C45/60 , C07C49/84 , C07D317/16 , C07C49/80
摘要： A process for producing a brominated acetal (represented by the formula 3) includes (a) brominating a trifluoromethyl-substituted acetophenone by Br2 in the presence of an alkylene diol. It is optional to produce a trifluoromethyl-substituted 2-alkoxyacetophenone derivative (represented by the formula 9) by (b) reacting the brominated acetal with a metal alkoxide, thereby converting the brominated acetal into an ether; and (c) hydrolyzing the ether in the presence of an acid catalyst to remove an acetal group from the ether, thereby producing the 2-alkoxyacetophenone derivative. Alternatively, the 2-alkoxyacetophenone can be produced by (a) reacting a trifluoromethyl-substituted phenacyl halide with an acetalization agent, thereby converting the phenacyl halide into an acetal; (b) reacting the acetal with a metal alkoxide, thereby converting the acetal into an ether; and (c) hydrolyzing the ether in the presence of an acid catalyst to remove the acetal group from the ether.
摘要翻译：制备溴化缩醛的方法（由式3表示）包括（a）在亚烷基二醇的存在下用Br 2 H 3溴化三氟甲基取代的苯乙酮。（b）使溴化缩醛与金属醇盐反应，从而将溴化缩醛转化成醚，任选地制备三氟甲基取代的2-烷氧基苯乙酮衍生物（由式9表示）和（c）在酸催化剂的存在下水解醚，以从乙醚中除去缩醛基，从而制备2-烷氧基苯乙酮衍生物。或者，2-烷氧基苯乙酮可以通过以下方法制备：（a）使三氟甲基取代的苯甲酰甲基卤化物与缩醛化剂反应，从而将苯甲酰甲酰卤转化成缩醛; （b）使缩醛与金属醇盐反应，从而将缩醛转化成醚; 和（c）在酸催化剂存在下水解该醚，以从乙醚中除去缩醛基。

26. 发明授权

US07795478B2 Process for producing optically active fluorobenzyl alcohol 有权
标题翻译：光学活性氟苄醇的制备方法
公开(公告)号：US07795478B2
公开(公告)日：2010-09-14
申请号：US12089882
申请日：2006-10-04
申请人： Akihiro Ishii , Koji Ueda , Manabu Yasumoto
发明人： Akihiro Ishii , Koji Ueda , Manabu Yasumoto
IPC分类号： C07C29/09
CPC分类号： C07C29/095 , C07B57/00 , C07B2200/07 , C07C67/08 , C07C67/60 , C07C33/40 , C07C33/22 , C07C69/80
摘要： A fluorine-containing benzaldehyde is reacted with an alkyl Grignard reagent to convert it to a magnesium alkoxide of racemic, fluorine-containing, benzyl alcohol, and subsequently the magnesium alkoxide is reacted with phthalic anhydride to obtain a phthalate half ester of racemic, fluorine-containing, benzyl alcohol, and the half ester is optically resolved by optically active 1-phenylethylamine, and then the ester group is hydrolyzed, thereby producing an optically active, fluorine-containing, benzyl alcohol.
摘要翻译：将含氟苯甲醛与烷基格氏试剂反应，将其转化成外消旋，含氟苄基醇的烷氧基镁，随后将烷氧基镁与邻苯二甲酸酐反应，得到外消旋，通过光学活性1-苯基乙胺光学拆分半酯，然后将酯基水解，从而制备光学活性的含氟苄基醇。

27. 发明申请

US20070142670A1 Optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy- substituted phenyl)alkylamine N-monoalkyl derivatives and process for producing same 有权
标题翻译：光学活性1-（氟，三氟甲基或三氟甲氧基取代的苯基）烷基胺N-单烷基衍生物及其制备方法
公开(公告)号：US20070142670A1
公开(公告)日：2007-06-21
申请号：US11705089
申请日：2007-02-12
申请人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
发明人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
IPC分类号： C07C211/26
CPC分类号： C07C209/62 , C07B2200/07 , C07C211/29 , C07C217/58 , C07C249/02 , C07C251/24
摘要： An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4 is produced by a process including (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent R2—X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, each of R1 and R2 independently represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, * represents a chiral carbon, and X represents a leaving group.
摘要翻译：由式4表示的光学活性1-（氟 - ，三氟甲基 - 或三氟甲氧基取代的苯基）烷基胺N-单烷基衍生物通过以下方法制备，该方法包括：（a）使由式1表示的光学活性仲胺与式烷基化剂R 2 -X在碱的存在下，由此将仲胺转化成由式3表示的光学活性叔胺; 和（b）使叔胺进行氢解，从而制备N-单烷基衍生物，其中R表示氟原子，三氟甲基或三氟甲氧基，n表示1〜5的整数，R 1 独立地表示碳原子数1〜6的烷基，Me表示甲基，Ar表示苯基或1-或2-萘基， *表示手性碳，X表示离去基团。

28. 发明申请

US20060281950A1 Process for producing optically active 1-alkyl-substituted 2,2,2-trifluoroethylamine 有权
标题翻译：光学活性1-烷基取代的2,2,2-三氟乙胺的制备方法
公开(公告)号：US20060281950A1
公开(公告)日：2006-12-14
申请号：US10560251
申请日：2004-06-08
申请人： Akihiro Ishii , Yokusu Kuriyama , Manabu Yasumoto , Masatomi Kanai , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
发明人： Akihiro Ishii , Yokusu Kuriyama , Manabu Yasumoto , Masatomi Kanai , Kenjin Inomiya , Takashi Ootsuka , Koji Ueda
IPC分类号： C07C211/02
CPC分类号： C07C209/62 , C07B2200/07 , C07C209/52 , C07C211/15 , C07C249/02 , C07C251/08
摘要： The present invention relates to a process for producing an optically active 1-alkyl-substituted 2,2,2-trifluoroethylamine, which is an important intermediate of medicines and agricultural chemicals, and which is represented by the formula [3] [in the formula R represents a lower alkyl group of a carbon and * represents an asymmetric carbon], or its salt by subjecting an optically active imine represented by the formula [1] to an asymmetric reduction under hydrogen atmosphere using a metal catalyst of Group VIII to convert it into an optically active secondary amine represented by the formula [2] and then by subjecting the secondary amine or its salt to hydrogenolysis. [Chem. 23]
摘要翻译：本发明涉及一种制备光学活性的1-烷基取代的2,2,2-三氟乙基胺的方法，它是药物和农药的重要中间体，由式[3] [式 R表示碳的低级烷基，*表示不对称碳]或其盐，通过使用式（1）表示的光学活性亚胺在氢气氛下使用VIII族金属催化剂进行不对称还原，将其转化为由式[2]表示的光学活性仲胺，然后通过使仲胺或其盐进行氢解。 [Chem。 23]

29. 发明授权

US07081551B2 Optically active (R)-1-(4-trifluoromethylphenyl)ethylamine 失效
标题翻译：光学活性（R）-1-（4-三氟甲基苯基）乙胺
公开(公告)号：US07081551B2
公开(公告)日：2006-07-25
申请号：US10442652
申请日：2003-05-21
申请人： Akihiro Ishii , Manabu Yasumoto , Yokusu Kuriyama , Masatomi Kanai , Kanjin Inomiya
发明人： Akihiro Ishii , Manabu Yasumoto , Yokusu Kuriyama , Masatomi Kanai , Kanjin Inomiya
IPC分类号： C07C209/28 , C07C251/24 , C07C211/03
CPC分类号： C07C251/24 , C07C211/29
摘要： Optically active (R)-1-(4-trifluoromethylphenyl)ethylamine is a novel compound as an important intermediate for medicines and agricultural chemicals. This compound can be obtained with high optical purity and high yield by a process including the steps of (a) a dehydrocondensation of 4′-(trifluoromethyl)acetophenone and an optically active (R)-1-phenylethylamine to obtain an optically active imine; (b) asymmetrically reducing the imine into an optically active secondary amine; (c) reacting the amine with an organic acid (phthalic acid or benzenesulfonic acid), thereby obtaining a product that is a phthalate of or benzenesulfonate of the amine; (d) subjecting the product of the step (c) to a hydrogenolysis, thereby obtaining a product that is a phthalate of or benzenesuilfonate of optically active (R)-1-(4-trifluoromethylphenyl)ethylamine; and (e) neutralizing the product of the step (d) into the optically active (R)-1-(4-trifluoromethylphenyl)ethylamine.
摘要翻译：光学活性（R）-1-（4-三氟甲基苯基）乙胺是一种新型化合物，作为药物和农药的重要中间体。通过包括以下步骤的（a）4' - （三氟甲基）苯乙酮和光学活性（R）-1-苯基乙胺的脱氢缩合得到光学活性亚胺，可以获得具有高光学纯度和高收率的该化合物。（b）将亚胺不对称地还原成光学活性仲胺; （c）使胺与有机酸（邻苯二甲酸或苯磺酸）反应，从而获得胺的邻苯二甲酸酯或苯磺酸盐的产物; （d）使步骤（c）的产物进行氢解，得到光学活性（R）-1-（4-三氟甲基苯基）乙胺的邻苯二甲酸酯或苯磺酸酯的产物; 和（e）将步骤（d）的产物中和到光学活性（R）-1-（4-三氟甲基苯基）乙胺中。

30. 发明授权

US06815559B2 Process for producing 3,3,3-trifluoro-2-hydroxypropionic acid or its derivative 失效
公开(公告)号：US06815559B2
公开(公告)日：2004-11-09
申请号：US10464838
申请日：2003-06-19
申请人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya
发明人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya
IPC分类号： C07C5300
CPC分类号： C07C51/295 , C07C59/115
摘要： The invention relates to a process for producing 3,3,3-trifluoro-2-hydroxypropionic acid. This process includes the step of (a) bringing a 1,1-dihalogeno-3,3,3-trifluoroacetone into contact with a basic aqueous solution. The obtained 3,3,3-trifluoro-2-hydroxypropionic acid may be reacted with a C1-C6 lower alcohol under an acidic condition, thereby producing a 3,3,3-trifluoro-2-hydroxypropionate. This propionate may be reacted with a hydride reducing agent (e.g., sodium borohydride), thereby producing 3,3,3-trifluoro-2-hydroxypropanol. These products (i.e., 3,3,3-trifluoro-2-hydroxypropionic acid and its derivatives) are important intermediates for medicines and liquid crystals.

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