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11. 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。

12. 发明授权

US5905174A Method for producing 3,3-dichloro-1,1,1-triflouroacetone 失效
标题翻译： 3,3-二氯-1,1,1-三氟丙酮的制备方法
公开(公告)号：US5905174A
公开(公告)日：1999-05-18
申请号：US60180
申请日：1998-04-15
申请人： Masatomi Kanai , Takashi Sakaya , Mineo Watanabe , Yoshihiko Goto , Ryo Nadano
发明人： Masatomi Kanai , Takashi Sakaya , Mineo Watanabe , Yoshihiko Goto , Ryo Nadano
IPC分类号： B01J27/08 , B01J27/125 , C07C45/63 , C07C45/82 , C07C45/83 , C07C45/00
CPC分类号： C07C45/82 , B01J27/08 , B01J27/125 , C07C45/63 , C07C45/83
摘要： The invention relates to a method for producing 3,3-dichloro-1,1,1-trifluoroacetone. This method includes a step of fluorinating pentachloroacetone by hydrogen fluoride in the presence of a fluorination catalyst. This fluorination may be conducted in a liquid phase in the presence of an antimony compound as the fluorination catalyst. Alternatively, the fluorination may be conducted in a gas phase in the presence of a fluorination catalyst which may be a fluorinated alumina or at least one compound of at least one metal selected from Al, Cr, Mn, Ni, and Co. The method is suited to an industrial scale production of 3,3-dichloro-1,1,1-trifluoroacetone. The invention further relates to another method for producing 3,3-dichloro-1,1,1-trifluoroacetone. This method includes a step of purifying a crude 3,3-dichloro-1,1,1-trifluoroacetone by a distillation in the presence of water, thereby to produce 3,3-dichloro-1,1,1-trifluoroacetone which is substantially free of organic matters other than 3,3-dichloro-1,1,1-trifluoroacetone. This crude 3,3-dichloro-1,1,1-trifluoroacetone may be the reaction products of the fluorination of pentachloroacetone in a gas phase. Due to the provision of the another method, 3,3-dichloro-1,1,1-trifluoroacetone can be produced with high yield.
摘要翻译：本发明涉及一种生产3,3-二氯-1,1,1-三氟丙酮的方法。该方法包括在氟化催化剂存在下用氟化氢氟化五氯丙酮的步骤。该氟化可以在作为氟化催化剂的锑化合物的存在下在液相中进行。或者，氟化可以在可以是氟化氧化铝或至少一种选自Al，Cr，Mn，Ni和Co的至少一种金属的化合物的氟化催化剂的存在下在气相中进行。该方法是适合工业规模生产3,3-二氯-1,1,1-三氟丙酮。本发明还涉及制备3,3-二氯-1,1,1-三氟丙酮的另一种方法。该方法包括在水存在下通过蒸馏纯化粗制3,3-二氯-1,1,1-三氟丙酮的步骤，从而产生3,3-二氯-1,1,1-三氟丙酮，其基本上不含3,3-二氯-1,1,1-三氟丙酮以外的有机物。该粗的3,3-二氯-1,1,1-三氟丙酮可以是五氯丙酮在气相中氟化的反应产物。由于提供另一种方法，可以高产率制备3,3-二氯-1,1,1-三氟丙酮。

13. 发明授权

US07459586B2 Optically active 1-aryl-2-fluoro-substituted ethylamine and method for producing same 有权
标题翻译：光活性1-芳基-2-氟取代的乙胺及其制备方法
公开(公告)号：US07459586B2
公开(公告)日：2008-12-02
申请号：US10591669
申请日：2005-02-21
申请人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Katsuhide Suto , Koji Ueda
发明人： Akihiro Ishii , Masatomi Kanai , Yokusu Kuriyama , Manabu Yasumoto , Kenjin Inomiya , Takashi Ootsuka , Katsuhide Suto , Koji Ueda
IPC分类号： C07C209/62 , C07C211/00 , C07C251/00
CPC分类号： C07C251/24 , C07C209/52 , C07C209/62 , C07C211/29 , C07C249/02
摘要： The present invention relates to a method of producing an optically active 1-aryl-2-fluoro-substituted ethylamine compound of the formula [2] or a salt thereof by hydrogenolysis of an optically active secondary amine compound of the formula [1] or a salt thereof in the presence of a transition metal catalyst of Group VIII[Chem. 59] [where Ar represents an aryl group; n represents an integer of 1 or 2; and * represents an asymmetric carbon] [Chem. 60] [where Ar represents an aryl group; n represents an integer of 1 or 2; and * represents an asymmetric carbon].
摘要翻译：本发明涉及通过氢解式[1]的光学活性仲胺化合物或式[1]的光学活性的1-芳基-2-氟取代的乙胺化合物或其盐，其盐在第VIII族的过渡金属催化剂存在下[Chem。 59]其中Ar表示芳基; n表示1或2的整数; 和*表示不对称碳] 60] [其中Ar表示芳基; n表示1或2的整数; 和*表示不对称碳]。

14. 发明授权

US07368609B2 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：US07368609B2
公开(公告)日：2008-05-06
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： C07C211/00
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。

15. 发明授权

US07189863B2 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：US07189863B2
公开(公告)日：2007-03-13
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： C07D319/06
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

16. 发明申请

US20050171363A1 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：US20050171363A1
公开(公告)日：2005-08-04
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： C07C43/315 , C07C45/57 , C07C45/59 , C07C45/60 , C07C49/84 , C07D317/16 , C07D317/22 , C07D323/02
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。

17. 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。

18. 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。

19. 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。

20. 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]

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