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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

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.

23. 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。

24. 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。

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