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    Optically active (R)-1-(4-trifluoromethylphenyl)ethylamine
    1.
    发明授权
    Optically active (R)-1-(4-trifluoromethylphenyl)ethylamine 失效
    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。

    Processing for producing 2′-deoxy-2′-fluorouridine
    4.
    发明授权
    Processing for producing 2′-deoxy-2′-fluorouridine 失效
    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。

    Optically active 1-(fluoro-, trifluoromethyl-or trifluoromethoxy-substituted phenyl) alkylamine n-monoalkyl derivatives and process for producing same
    5.
    发明授权
    Optically active 1-(fluoro-, trifluoromethyl-or trifluoromethoxy-substituted phenyl) alkylamine n-monoalkyl derivatives and process for producing same 有权
    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。

    Process for producing 2'-deoxy-2'-fluorouridine
    6.
    发明申请
    Process for producing 2'-deoxy-2'-fluorouridine 失效
    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。

    Process for producing trifluoromethyl-substituted 2-alkoxyacetophenone derivatives
    7.
    发明申请
    Process for producing trifluoromethyl-substituted 2-alkoxyacetophenone derivatives 失效
    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。

    Process for producing trifluoromethyl- substituted 2- alkoxyacetophenone derivatives
    8.
    发明授权
    Process for producing trifluoromethyl- substituted 2- alkoxyacetophenone derivatives 有权
    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。

    Optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy- substituted phenyl)alkylamine N-monoalkyl derivatives and process for producing same
    9.
    发明申请
    Optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy- substituted phenyl)alkylamine N-monoalkyl derivatives and process for producing same 有权
    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。