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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明申请

US20070191639A1 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：US20070191639A1
公开(公告)日：2007-08-16
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： C07C209/26
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]。

6. 发明授权

US07393979B2 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：US07393979B2
公开(公告)日：2008-07-01
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： C07C209/62 , C07C211/05
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]

7. 发明授权

US07388094B2 Processing for producing 2′-deoxy-2′-fluorouridine 失效
标题翻译： 2'-脱氧-2'-氟尿苷的制备方法
公开(公告)号：US07388094B2
公开(公告)日：2008-06-17
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： C07H19/073
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。

8. 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。

9. 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。

10. 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。

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