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    IMPROVED PROCESS FOR THE PREPARATION OF ARYLPYRIDINYL COMPOUNDS
    2.
    发明申请
    IMPROVED PROCESS FOR THE PREPARATION OF ARYLPYRIDINYL COMPOUNDS 审中-公开
    制备芳基吡啶化合物的改进方法

    公开(公告)号：US20120157687A1

    公开(公告)日：2012-06-21

    申请号：US13380611

    申请日：2010-06-24

    申请人： Roberto Scrocchi ,  Fedeli Palma ,  Argese Maria ,  Guazzi Giuseppe

    发明人： Roberto Scrocchi ,  Fedeli Palma ,  Argese Maria ,  Guazzi Giuseppe

    IPC分类号： C07D213/42 ,  C07D213/48

    CPC分类号： C07D213/48 ,  C07D213/42

    摘要： A process is described for the preparation of arylpyridine compounds by aryl-aryl cross-coupling reactions between a halopyridine and an arylmagnesium halide carried out in the presence of a catalytic amount of a zinc salt and a catalytic amount of palladium complex with a bidentate phosphine. The zinc salt is preferably selected from ZnCl2, ZnBr2 and/or Zn(OAc)2, while the palladium complex with a bidentate phosphine is preferably selected from the group of (1,2-Bis(diphenylphosphino)ethane)palladium(II) chloride, (1,3-Bis(diphenylphosphino)propane)palladium(II) chloride and (1,4-Bis(diphenylphosphino)butane)palladium(II) chloride. Most preferred is (1,2-Bis(diphenylphosphino)ethane)palladium(II) chloride. It is thus possible to obtain molar yields higher than 95% calculated on the arylmagnesium halide and a catalyticity less than 1:1500. The process is particularly suitable for the preparation of 4-(2′-pyridyl)benzaldehyde which can then effectively been converted to N1-(t-butoxycarbonyl)-N2-(4-(2′pyridyl)benzyl)hydrazine.

    摘要翻译： 描述了通过在催化量的锌盐和催化量的钯络合物与二齿膦存在下进行的卤代吡啶和芳基卤化镁之间的芳基 - 芳基交叉偶联反应制备芳基吡啶化合物的方法。 锌盐优选选自ZnCl 2，ZnBr 2和/或Zn（OAc）2，而具有二齿膦的钯络合物优选选自（1,2-双（二苯基膦基）乙烷）氯化钯（II） ，（1,3-双（二苯基膦基）丙烷）氯化钯（II）和（1,4-双（二苯基膦基）丁烷）氯化钯（II）。 最优选的是（1,2-双（二苯基膦基）乙烷）氯化钯（II）。 因此可以获得高于95％的摩尔收率，其计算方法为芳基卤化镁和催化性小于1:1500。 该方法特别适用于4-（2'-吡啶基）苯甲醛的制备，然后可有效地将其转化为N1-（叔丁氧基羰基）-N2-（4-（2'-吡啶基）苄基）肼。

    Process for producing heterocyclic aldehyde
    3.
    发明申请
    Process for producing heterocyclic aldehyde 有权
    制备杂环醛的方法

    公开(公告)号：US20050124807A1

    公开(公告)日：2005-06-09

    申请号：US10509228

    申请日：2003-03-25

    申请人： Yasuhiro Shiomi ,  Osamu Uno ,  Akio Ohta ,  Takeshi Sunakami

    发明人： Yasuhiro Shiomi ,  Osamu Uno ,  Akio Ohta ,  Takeshi Sunakami

    IPC分类号： C07D213/48 ,  C07D333/18 ,  C07D213/46 ,  C07D241/02

    CPC分类号： C07D213/48

    摘要： The present invention provides a process for preparing a heterocyclic aldehyde by oxidizing a heterocyclic alcohol with high selectivity and high yield. Specifically, the heterocyclic aldehyde is prepared by reacting a heterocyclic compound having at least one hydroxymethyl group bonded to a carbon atom of a heterocyclic ring with a hypohalogenous acid salt in the presence of a base to oxidize the hydroxymethyl group, wherein reaction is conducted in the co-presence of a 2,2,6,6-tetramethylpiperidine-1-oxyl derivative having at least two 2,2,6,6-tetramethylpiperidine-1-oxyl-4-yl groups.

    摘要翻译： 本发明提供了通过以高选择性和高收率氧化杂环醇制备杂环醛的方法。 具体地说，杂环醛通过使具有至少一个羟基甲基与杂环的碳原子键合的杂环化合物与低级卤酸酸盐在碱的存在下反应来制备，以氧化羟甲基，其中反应在 具有至少两个2,2,6,6-四甲基哌啶-1-氧基-4-基的2,2,6,6-四甲基哌啶-1-氧基衍生物的共存。

    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：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。