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    2-phenylpyridine derivative and production method thereof
    1.
    发明授权
    2-phenylpyridine derivative and production method thereof 有权
    2-苯基吡啶衍生物及其制备方法

    公开(公告)号：US06242608B1

    公开(公告)日：2001-06-05

    申请号：US09602031

    申请日：2000-06-23

    申请人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D21170

    CPC分类号： C07D213/42 ,  C07D213/26 ,  C07D213/48

    摘要： A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

    摘要翻译： 一系列能产生下式的化合物（A）的中间体的化合物，其为抗HIV药物及其制备方法。 具体地说，4-（吡啶-2-基）苯甲醛腙，该化合物的制备方法，以及由该化合物制备N-（叔丁氧基羰基）-N' - [4-（吡啶-2-基） 苯基亚甲基]肼。 此外，2-（4-溴甲基苯基）吡啶，2-（4-二溴甲基苯基）吡啶及其盐的盐，这些化合物的制备方法和得到4-（吡啶-2-基）苯甲醛的制备方法 是来自这些化合物的4-（吡啶-2-基）苯甲醛腙的生产中间体。

    2-phenylpyridine derivative and production method thereof
    3.
    发明授权
    2-phenylpyridine derivative and production method thereof 有权
    2-苯基吡啶衍生物及其制备方法

    公开(公告)号：US6147218A

    公开(公告)日：2000-11-14

    申请号：US370636

    申请日：1999-08-06

    申请人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D213/26 ,  C07D213/42 ,  C07D213/48 ,  C07D213/02

    CPC分类号： C07D213/42 ,  C07D213/26 ,  C07D213/48

    摘要： A series of compounds capable of deriving an intermediate for the production of a compound (A) of the following formula, ##STR1## which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N'-[4-(pyridin-2-yl)phenylmethyhidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

    摘要翻译： 一系列能产生下式的化合物（A）的中间体的化合物，其为抗HIV药物及其制备方法。 具体地说，4-（吡啶-2-基）苯甲醛腙，该化合物的制备方法，以及由该化合物制备N-（叔丁氧基羰基）-N' - [4-（吡啶-2-基） 苯基亚甲基]肼。 此外，2-（4-溴甲基苯基）吡啶，2-（4-二溴甲基苯基）吡啶及其盐的盐，这些化合物的制备方法和得到4-（吡啶-2-基）苯甲醛的制备方法 是来自这些化合物的4-（吡啶-2-基）苯甲醛腙的生产中间体。

    2-phenylpyridine derivative and production method thereof
    4.
    发明授权
    2-phenylpyridine derivative and production method thereof 有权
    2-苯基吡啶衍生物及其制备方法

    公开(公告)号：US06268503B1

    公开(公告)日：2001-07-31

    申请号：US09611991

    申请日：2000-07-07

    申请人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Kozo Matsui ,  Kiyoshi Sugi ,  Yoshihide Umemoto ,  Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D21326

    CPC分类号： C07D213/42 ,  C07D213/26 ,  C07D213/48

    摘要： A series of compounds capable of deriving an intermediate for the production of compound (A) of the following formula, which is an anti-HIV drug, and a production method thereof. To be specific, 4-(pyridin-2-yl)benzaldehyde hydrazone, a production method of this compound, and a production method from this compound to N-(tert-butoxycarbonyl)-N′-[4-(pyridin-2-yl)phenylmethylidene]hydrazine. In addition, a salt of 2-(4-bromomethylphenyl)pyridine, 2-(4-dibromomethylphenyl)pyridine and a salt thereof, production methods of these compounds, and production methods to derive 4-(pyridin-2-yl)benzaldehyde which is a production intermediate for 4-(pyridin-2-yl)benzaldehyde hydrazone from these compounds.

    摘要翻译： 一系列能够得到用于制备作为抗HIV药物的下式化合物（A）的中间体的化合物及其制备方法。 具体地说，4-（吡啶-2-基）苯甲醛腙，该化合物的制备方法，以及由该化合物制备N-（叔丁氧基羰基）-N' - [4-（吡啶-2-基） 苯基亚甲基]肼。 此外，2-（4-溴甲基苯基）吡啶，2-（4-二溴甲基苯基）吡啶及其盐的盐，这些化合物的制备方法和得到4-（吡啶-2-基）苯甲醛的制备方法 是来自这些化合物的4-（吡啶-2-基）苯甲醛腙的生产中间体。

    Production method of hydrazine derivative
    5.
    发明授权
    Production method of hydrazine derivative 有权
    肼衍生物的制备方法

    公开(公告)号：US06376678B1

    公开(公告)日：2002-04-23

    申请号：US09521058

    申请日：2000-03-08

    申请人： Kiyoshi Sugi ,  Kozo Matsui ,  Tetsuya Shintaku ,  Nobushige Itaya

    发明人： Kiyoshi Sugi ,  Kozo Matsui ,  Tetsuya Shintaku ,  Nobushige Itaya

    IPC分类号： C07D21170

    CPC分类号： C07D213/06 ,  C07D213/42

    摘要： A production method of hydrazine derivative having a group of the formula (II) which comprises subjecting a hydrazone derivative having a group of the formula (I) to catalytic reduction and deactivating the reduction catalyst contained in the reaction mixture thereof. According to the production method of the present invention, which is industrially superior, hydrazine derivative (II) stable even in a solution state can be produced

    摘要翻译： 具有式（II）基团的肼衍生物的制备方法，其包括将具有式（I）的基团的腙衍生物进行催化还原和使其反应混合物中所含的还原催化剂失活。 根据工业上优越的本发明的制造方法，可以制造即使在溶液状态下稳定的肼衍生物（II）

    Method for producing hydrazine derivative
    6.
    发明授权
    Method for producing hydrazine derivative 有权
    肼衍生物的制备方法

    公开(公告)号：US06365745B1

    公开(公告)日：2002-04-02

    申请号：US09905442

    申请日：2001-07-13

    申请人： Kozo Matsui ,  Kiyoshi Sugi ,  Hiromi Suga ,  Nobushige Itaya

    发明人： Kozo Matsui ,  Kiyoshi Sugi ,  Hiromi Suga ,  Nobushige Itaya

    IPC分类号： C07D21304

    CPC分类号： C07C281/02 ,  C07C241/04 ,  C07C243/32

    摘要： The present invention provides a method for producing a hydrazine derivative of the formula [2]: wherein R1 is alkyl group having 1-12 carbon atoms and the like, R2 is alkyl group having 1-12 carbon atoms and the like, and Ar is phenylene group and the like, from a hydrazone derivative of the formula [1] wherein R1, R2 and Ar are as defined above, in the presence of at least one base selected from the group consisting of an organic base and an inorganic base, and a metal hydrogenating catalyst. By this method, reduction proceeds selectively and a hydrogenolysis reaction (side reaction) can be suppressed.

    摘要翻译： 本发明提供式[2]的肼衍生物的制造方法，其中R1为具有1-12个碳原子的烷基等，R2为具有1-12个碳原子的烷基等，Ar为 亚苯基等，由式[1]的腙衍生物，其中R 1，R 2和Ar如上定义，在至少一种选自有机碱和无机碱的碱的存在下，和 金属氢化催化剂。 通过该方法，可以选择性地还原还原，可以抑制氢解反应（副反应）。

    Process for producing 2'-(1h-tetrazol-5-yl)biphenyl-4-carbaldehyde
    8.
    发明申请
    Process for producing 2'-(1h-tetrazol-5-yl)biphenyl-4-carbaldehyde 审中-公开
    制备2' - （1h-四唑-5-基）联苯-4-甲醛的方法

    公开(公告)号：US20070072923A1

    公开(公告)日：2007-03-29

    申请号：US10595122

    申请日：2004-09-01

    申请人： Nobushige Itaya ,  Kozo Matsui ,  Yutaka Ohtani ,  Hiroki Ueno ,  Toshikazu Kaneko

    发明人： Nobushige Itaya ,  Kozo Matsui ,  Yutaka Ohtani ,  Hiroki Ueno ,  Toshikazu Kaneko

    IPC分类号： A61K31/41 ,  C07D257/02

    CPC分类号： C07D257/04

    摘要： The present invention provides a process for producing 2′-(1H-tetrazol-5-yl)biphenyl-4-carbaldehyde which comprises reacting 2′-cyanobiphenyl-4-carbaldehyde with a salt of azide; a process for producing a highly pure crystal of 2′-(1H-tetrazol-5-yl)biphenyl-4-carbaldehyde which comprises reacting 2′-cyanobiphenyl-4-carbaldehyde with a salt of azide, obtaining a crystal of 2′-(1H-tetrazol-5-yl)biphenyl-4-carbaldehyde, dissolving said crystal obtained and recrystallizing a highly pure crystal in tetrahydrofuran; and the like. According to the present process, 2′-(1H-tetrazol-5-yl)biphenyl-4-carbaldehyde which is useful as a synthetic intermediate of medicines can be produced in a short process at high yield and high purity.

    摘要翻译： 本发明提供2' - （1H-四唑-5-基）联苯-4-甲醛的制备方法，其包括使2'-氰基联苯-4-甲醛与叠氮化物的盐反应; 2' - （1H-四唑-5-基）联苯-4-甲醛的高纯度晶体的制造方法，其包括使2'-氰基联苯-4-甲醛与叠氮化物的盐反应，得到2'- （1H-四唑-5-基）联苯-4-甲醛，将所得晶体溶解并将高纯度结晶重结晶于四氢呋喃中; 等等。 根据本发明，可以以高产率和高纯度的短时间制备可用作药物合成中间体的2' - （1H-四唑-5-基）联苯-4-甲醛。