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21. 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。

22. 发明授权

US06797842B2 Process for producing optically active 1-(fluoro- or trifluoromethyl-substituted phenyl) ethylamine and process for purifying same 失效
标题翻译：光学活性1-（氟代或三氟甲基取代的苯基）乙胺的制备方法及其纯化方法
公开(公告)号：US06797842B2
公开(公告)日：2004-09-28
申请号：US09853085
申请日：2001-05-11
申请人： Akihiro Ishii , Manabu Yasumoto , Yokusu Kuriyama , Masatomi Kanai , Takashi Hayami
发明人： Akihiro Ishii , Manabu Yasumoto , Yokusu Kuriyama , Masatomi Kanai , Takashi Hayami
IPC分类号： C07C21100
CPC分类号： C07C209/52 , C07B2200/07 , C07C211/29
摘要： An optically active 1-(fluoro- or trifluoromethyl-substituted phenyl)ethylamine is produced with high optical purity and in an industrially simple and efficient manner by asymmetrically reducing an optically active imine, obtained by dehydration and condensation of a fluoro- or trifluoromethyl-substituted phenylmethyl ketone and an optically active primary amine under acidic conditions, using a hydride reducing agent to convert to an optically active secondary amine, and subjecting the secondary amine or its salt of an inorganic acid or organic acid to hydrogenolysis. In addition, an optically active 1-(fluoro- or trifluoromethyl-substituted phenyl)ethylamine is purified to an even higher optical purity in an industrially simple and efficient manner by converting the optically active secondary amine of the synthetic intermediate obtained by asymmetric reduction, or an optically active 1-(3,5-bis-trifluoromethylphenyl)ethylamine, one of the target compounds, to an inorganic or organic acid salt followed by recrystallization purification. This ethylamine is an important intermediate of pharmaceuticals and agricultural chemicals.
摘要翻译：以光学纯度高的光学活性的1-（氟代或三氟甲基取代的苯基）乙胺，以工业上简单有效的方式，通过不对称地还原通过氟 - 或三氟甲基取代的脱水和缩合得到的光学活性亚胺苯甲基酮和光学活性伯胺在酸性条件下，使用氢化物还原剂转化成光学活性仲胺，并使无机酸或有机酸的仲胺或其盐进行氢解。此外，通过将通过不对称还原得到的合成中间体的光学活性仲胺转化成光学活性的1-（氟代或三氟甲基取代的苯基）乙胺，以工业简单且有效的方式纯化至更高的光学纯度，或光学活性的1-（3,5-双三氟甲基苯基）乙胺，一种目标化合物，与无机或有机酸盐接着重结晶纯化。该乙胺是药物和农药的重要中间体。

23. 发明授权

US06639100B2 Process for producing 4,4,4,-trifluoro-3-hydroxybutyric acid 失效
标题翻译：制备4,4,4-三氟-3-羟基丁酸的方法
公开(公告)号：US06639100B2
公开(公告)日：2003-10-28
申请号：US10212840
申请日：2002-08-07
申请人： Akihiro Ishii , Masatomi Kanai , Takashi Hayami , Katsuyoshi Shibata , Masaki Matsui , Kazumasa Funabiki , Yokusu Kuriyama , Manabu Yasumoto
发明人： Akihiro Ishii , Masatomi Kanai , Takashi Hayami , Katsuyoshi Shibata , Masaki Matsui , Kazumasa Funabiki , Yokusu Kuriyama , Manabu Yasumoto
IPC分类号： C07C6963
CPC分类号： C07C69/675 , C07B2200/07 , C07C29/143 , C07C45/516 , C07C45/78 , C07C45/81 , C07C49/82 , C07C49/84 , C07C31/42
摘要： A process for producing an optically active perfluoroalkylcarbinol by reacting an optically active imine with a hemiacetal or hydrate of a perfluoroalkylaldehyde to obtain a condensate, and hydrolyzing the condensate under acidic conditions. Optical purity of optically active 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone compounds may be increased by precipitating and removing a racemic crystal, and also recrystallizing the compound. Novel compounds include optically active and inactive 4,4,4-trifluoro-3-hydroxybutanoic aryl esters. A process for producing optically active or incactive 4,4,4-trifluoro-3-hydroxybutyric acid aryl esters includes oxidizing an optically active or inactive 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone. Optical purity of optically active aryl esters may be increased by recrystallization. Optically active 4,4,4-trifluoro-1,3-butanediol may be produced by reducing the optically active aryl ester with a hydride. Optically active or inactive 4,4,4-trifluoro-3-hydroxybutyric acid alkyl esters are produced by reacting optically active or inactive aryl esters with lower alcohols under acid conditions.
摘要翻译：通过使光学活性亚胺与全氟烷基醛的半缩醛或水合物反应得到缩合物，并在酸性条件下水解缩合物，制备光学活性全氟烷基甲醇的方法。光学活性的4,4,4-三氟-3-羟基-1-芳基-1-丁酮化合物的光学纯度可以通过沉淀和除去外消旋晶体而增加，也可以使化合物重结晶。新型化合物包括光学活性和无活性的4,4,4-三氟-3-羟基丁酸芳酯。制备光学活性或不活泼的4,4,4-三氟-3-羟基丁酸芳基酯的方法包括氧化光学活性或无活性的4,4,4-三氟-3-羟基-1-芳基-1-丁酮。光学活性芳基酯的光学纯度可通过重结晶而增加。可以通过用氢化物还原光学活性芳基酯来制备光学活性的4,4,4-三氟-1,3-丁二醇。光学活性或无活性的4,4,4-三氟-3-羟基丁酸烷基酯是通过在酸性条件下使光学活性或惰性芳基酯与低级醇反应来制备的。

24. 发明授权

US06833468B2 Process for producing 4,4,4-trifluoro-3-hydroxybutyric acid derivatives 失效
标题翻译：制备4,4,4-三氟-3-羟基丁酸衍生物的方法
公开(公告)号：US06833468B2
公开(公告)日：2004-12-21
申请号：US10202833
申请日：2002-07-26
申请人： Akihiro Ishii , Masatomi Kanai , Takashi Hayami , Katsuyoshi Shibata , Masaki Matsui , Kazumasa Funabiki , Yokusu Kuriyama , Manabu Yasumoto
发明人： Akihiro Ishii , Masatomi Kanai , Takashi Hayami , Katsuyoshi Shibata , Masaki Matsui , Kazumasa Funabiki , Yokusu Kuriyama , Manabu Yasumoto
IPC分类号： C07C6900
CPC分类号： C07C69/675 , C07B2200/07 , C07C29/143 , C07C45/516 , C07C45/78 , C07C45/81 , C07C49/82 , C07C49/84 , C07C31/42
摘要： A first process for producing an optically active perfluoroalklylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybotanoic aryl ester derivatives. A fourth or fifth process for producing an optically active and inactive 4,4,4-trifluoro-3-hydroxybutyric acid aryl ester derivative includes oxidizing an optically active or optically inactive 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative. A sixth process for increasing optical purity of the optically active aryl ester derivative includes recrystallizing the derivative. A seventh process for producing an optically active 4,4,4-trifluoro-3-butanediol includes reducing the optically active aryl ester derivative by a hydride. An eighth or ninth process for producing an optically active or inactive 4,4,4-trifluoro-3-hydroxybutyric acid alkyl ester derivative includes reacting under an acid condition the optically active or optically inactive aryl ester derivative with a lower alcohol. It is possible to suitably combine at least two of the first to ninth processes.
摘要翻译：制备光学活性全氟烷基甲醇基衍生物的第一种方法包括（a）使光学活性亚胺与全氟烷基醛的半缩醛化合物或全氟烷基醛的水合物反应得到缩合物; 和（b）在酸性条件下水解冷凝物。提高光学活性4,4,4-三氟-3-羟基-1-芳基-1-丁酮衍生物的光学纯度的第二种方法包括（a）衍生物沉淀衍生物的外消旋晶体; 和（b）从衍生物中除去外消旋晶体。提高丁酮衍生物的光学纯度的第三种方法包括使衍生物重结晶。新型化合物是光学活性和无活性的4,4,4-三氟-3-羟基伯烷基酯衍生物。用于制备光学活性和无活性的4,4,4-三氟-3-羟基丁酸芳基酯衍生物的第四或第五种方法包括将光学活性或光学活性的4,4,4-三氟-3-羟基-1-芳基 -1-丁酮衍生物。提高光学活性芳基酯衍生物的光学纯度的第六种方法包括使衍生物重结晶。制备光学活性4,4,4-三氟-3-丁二醇的第七种方法包括用氢化物还原光学活性芳基酯衍生物。用于制备光学活性或无活性的4,4,4-三氟-3-羟基丁酸烷基酯衍生物的第八或第九方法包括在酸性条件下使光学活性或光学惰性的芳基酯衍生物与低级醇反应。可以适当地组合第一至第九工艺中的至少两个。

25. 发明授权

US06642409B2 Process for producing 4,4,4-trifluoro-3-hydroxybutyric acid derivatives 失效
标题翻译：制备4,4,4-三氟-3-羟基丁酸衍生物的方法
公开(公告)号：US06642409B2
公开(公告)日：2003-11-04
申请号：US09770671
申请日：2001-01-29
申请人： Akihiro Ishii , Masatomi Kanai , Takashi Hayami , Katsuyoshi Shibata , Masaki Matsui , Kazumasa Funabiki , Yokusu Kuriyama , Manabu Yasumoto
发明人： Akihiro Ishii , Masatomi Kanai , Takashi Hayami , Katsuyoshi Shibata , Masaki Matsui , Kazumasa Funabiki , Yokusu Kuriyama , Manabu Yasumoto
IPC分类号： C07C6993
CPC分类号： C07C69/675 , C07B2200/07 , C07C29/143 , C07C45/516 , C07C45/78 , C07C45/81 , C07C49/82 , C07C49/84 , C07C31/42
摘要： A first process for producing an optically active perfluoroalklylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfinoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative (includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybotanoic aryl ester derivatives. A fourth or fifth process for producing an optically active and inactive 4,4,4-trifloro-3-hydroxybutyric acid aryl ester derivative includes oxidizing an optically active or optically inactive 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative. A sixth process for increasing optical purity of the optically active aryl ester derivative includes recrystallizing the derivative. A seventh process for producing an optically active 4,4,4-trifluoro-3-butanediol includes reducing the optically active aryl ester derivative by a hydride. An eighth or ninth process for producing an optically active or inactive 4,4,4-trifluoro-3-hydroxybutyric acid alkyl ester derivative includes reacting under an acid condition the optically active or optically inactive aryl ester derivative with a lower alcohol. It is possible to suitably combine at least two of the first to ninth processes.
摘要翻译：制备光学活性全氟烷基甲醇基衍生物的第一种方法包括（a）使光学活性亚胺与全氟烷基醛的半缩醛化合物或全氟烷基醛的水合物反应得到一种缩合物; 和（b）在酸性条件下水解冷凝物。提高光学活性4,4,4-三氟-3-羟基-1-芳基-1-丁酮衍生物的光学纯度的第二种方法包括（a）衍生物沉淀衍生物的外消旋晶体; 和（b）从衍生物中除去外消旋晶体。提供丁酮衍生物的光学纯度的第三种方法（包括重结晶衍生物）新型化合物是光学活性和无活性的4,4,4-三氟-3-羟基己酸芳基酯衍生物。第四或第五种光学活性和不活泼的4,4,4-三氟-3-羟基丁酸芳酯衍生物包括氧化光学活性或光学活性的4,4,4-三氟-3-羟基-1-芳基-1-丁酮衍生物。第六种增加方法光学活性芳基酯衍生物的光学纯度包括使该衍生物重结晶。第四种制备光学活性4,4,4-三氟-3-丁二醇的方法包括用氢化物还原光学活性芳基酯衍生物，第八或第九种方法用于制备光学活性或无活性的4,4,4-三氟-3-羟基丁酸烷基酯衍生物包括在酸性条件下使光学活性或光学惰性的芳基酯衍生物 e与低级酒精。可以适当地组合第一至第九工艺中的至少两个。

26. 发明申请

US20100267940A1 Method for Producing 4-Deoxy-4-Fluoro-D-Glucose Derivative 审中-公开
标题翻译：生产4-脱氧-4-氟-D-葡萄糖衍生物的方法
公开(公告)号：US20100267940A1
公开(公告)日：2010-10-21
申请号：US12747071
申请日：2008-11-26
申请人： Akihiro Ishii , Manabu Yasumoto , Takashi Ootsuka , Yasuko Nigorikawa
发明人： Akihiro Ishii , Manabu Yasumoto , Takashi Ootsuka , Yasuko Nigorikawa
IPC分类号： C07H15/207 , C07H1/00
CPC分类号： C07H1/00 , C07H5/02 , C07H15/04
摘要： There is disclosed a method for producing a 4-deoxy-4-fluoro-D-glucose derivative by reacting a D-galactose derivative with either sulfuryl fluoride (SO2F2), trifluoromethanesulfonyl fluoride (CF3SO2F) or perfluorobutanesulfonyl fluoride (C4F9SO2F) in the presence of an organic base or in the presence of an organic base and a salt or complex of an organic base and hydrogen fluoride.
摘要翻译：公开了通过使D-半乳糖衍生物与硫酰氟（SO 2 F 2），三氟甲磺酰氟（CF 3 SO 2 F）或全氟丁磺酰氟（C 4 F 9 SO 2 F）在存在下反应生成4-脱氧-4-氟-D-葡萄糖衍生物的方法有机碱或有机碱和有机碱和氟化氢的盐或络合物存在下进行。

27. 发明申请

US20110251403A1 Method for Manufacturing Hydroxyl Group Substitution Product 审中-公开
标题翻译：羟基取代产物的制备方法
公开(公告)号：US20110251403A1
公开(公告)日：2011-10-13
申请号：US13140307
申请日：2009-12-15
申请人： Akihiro Ishii , Manabu Yasumoto , Koji Ueda
发明人： Akihiro Ishii , Manabu Yasumoto , Koji Ueda
IPC分类号： C07D207/16 , C07C67/327
CPC分类号： C07D207/16 , C07C67/307 , C07C67/31 , C07C69/63 , C07C69/68
摘要： In the present invention, a hydroxyl group substitution product is manufactured by reaction of an alcohol with sulfuryl fluoride (SO2F2) in the presence of an organic base and a nucleophile (X−). The present invention is thus effective as an industrial manufacturing method that uses a relatively cheap reagent suitable for large-scale applications and can be accomplished in a simple process with easy purification operation and less waste generation and is suitably applicable for manufacturing of optically active hydroxyl group substitution products, notably optically active α-hydroxyl group substitution ester and optically active 4-hydroxyl group substitution proline. The manufacturing method of the present invention solves all of the prior art problems and can be applied for industrial uses.
摘要翻译：在本发明中，通过在有机碱和亲核体（X）的存在下，通过醇与硫酰氟（SO 2 F 2）的反应制备羟基取代产物。因此，本发明作为工业制造方法是有效的，其使用适合于大规模应用的相对便宜的试剂，并且可以在简单的方法中实现，容易的纯化操作和较少的废物产生，并且适用于制造光学活性羟基取代产物，特别是光学活性的α-羟基取代酯和光学活性的4-羟基取代脯氨酸。本发明的制造方法解决了所有现有技术的问题，可以应用于工业用途。

28. 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。

29. 发明申请

US20090240087A1 Process for Producing Optically Active Fluorobenzyl Alcohol 有权
标题翻译：生产光活性氟苄醇的方法
公开(公告)号：US20090240087A1
公开(公告)日：2009-09-24
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： C07C33/46
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。

30. 发明授权

US09040745B2 Process for producing fluorosulfuric acid aromatic-ring esters 有权
标题翻译：制备氟代硫酸芳环酯的方法
公开(公告)号：US09040745B2
公开(公告)日：2015-05-26
申请号：US14128362
申请日：2012-06-15
申请人： Akihiro Ishii , Takehisa Ishimaru , Takako Yamazaki , Manabu Yasumoto
发明人： Akihiro Ishii , Takehisa Ishimaru , Takako Yamazaki , Manabu Yasumoto
IPC分类号： C07C303/24
CPC分类号： C07C303/24 , C07C305/26
摘要： A production process of a fluorosulfuric acid aromatic-ring ester according to the present invention includes reaction of an aromatic-ring hydroxyl compound with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine except pyridine and methylpyridine. The sulfuryl fluoride, used as the reactant in the production process according to the present invention, is widely adapted as a fumigant and is easily available on a large scale. Further, the target compound can be obtained rapidly with a high yield under moderate reaction conditions in the production process according to the present invention. In this way, all of the prior art problems can be solved in the production process according to the present invention. The production process according to the present invention is thus particularly useful for industrial production of the fluorosulfuric acid aromatic-ring ester.
摘要翻译：根据本发明的氟代硫酸芳环酯的制备方法包括在除吡啶和甲基吡啶之外的叔胺存在下，芳环羟基化合物与硫酰氟（SO 2 F 2）的反应。在根据本发明的生产方法中用作反应物的硫酰氟被广泛地用作熏蒸剂，并且容易获得大量。此外，在本发明的制造方法中，在中等反应条件下，可以快速获得目标化合物。以这种方式，可以在根据本发明的制造方法中解决所有现有技术问题。因此，本发明的制造方法特别适用于氟代硫酸芳香环酯的工业化生产。

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