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87 条记录 (耗时 0.026 秒)

    Production method of epoxide crystal
    62.
    发明授权
    Production method of epoxide crystal 失效
    环氧化物晶体的制备方法

    公开(公告)号：US06764545B2

    公开(公告)日：2004-07-20

    申请号：US10011304

    申请日：2001-12-11

    申请人： Yuichi Suzuki ,  Naoko Hirose ,  Tomoyuki Onishi ,  Kunisuke Izawa

    发明人： Yuichi Suzuki ,  Naoko Hirose ,  Tomoyuki Onishi ,  Kunisuke Izawa

    IPC分类号： C30B708

    CPC分类号： C07D301/36

    摘要： The present invention provides a production method including adding water to a solution of (2R,3S)-3-tert-butoxycarbonylamino-1,2-epoxy-4-phenylbutane ((2R,3S)-epoxide compound) or (2S,3R)-3-tert-butoxycarbonylamino-1,2-epoxy-4-phenylbutane ((2S,3R)-epoxide compound) in a polar solvent to allow crystallization, whereby to produce crystals of the (2R,3S)-epoxide compound or the (2S,3R)-epoxide compound conveniently in a high yield by an industrial production method without requiring an extremely low temperature.

    摘要翻译： 本发明提供一种制备方法，其包括向（2R，3S）-3-叔丁氧基羰基氨基-1,2-环氧-4-苯基丁烷（（2R，3S） - 环氧化合物）或（2S，3R ）-3-叔丁氧基羰基氨基-1,2-环氧-4-苯基丁烷（（2S，3R） - 环氧化合物）在极性溶剂中进行结晶，从而得到（2R，3S） - 环氧化合物的晶体或 （2S，3R） - 环氧化合物通过工业生产方法方便地高收率，而不需要极低的温度。

    Methods for producing nucleoside derivatives and intermediates therefor
    64.
    发明授权
    Methods for producing nucleoside derivatives and intermediates therefor 失效
    制备核苷衍生物的方法及其中间体

    公开(公告)号：US06500946B1

    公开(公告)日：2002-12-31

    申请号：US09567980

    申请日：2000-05-10

    申请人： Satoshi Takamatsu ,  Satoshi Katayama ,  Naoko Hirose ,  Kunisuke Izawa ,  Tokumi Maruyama

    发明人： Satoshi Takamatsu ,  Satoshi Katayama ,  Naoko Hirose ,  Kunisuke Izawa ,  Tokumi Maruyama

    IPC分类号： C07H1919

    CPC分类号： C07D473/00 ,  C07H19/16

    摘要： Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even substrates, of which the 3′-position of the saccharide moiety is deoxylated, can be substituted at the 2′-position at an extremely high yield. Specifically, by subjecting a 3′-deoxy derivative of inosine to 6-halogenation to give a 6-halide of the derivative, and then subjecting it to 2′-deoxylation/substitution with a fluorine atom or the like, followed by further subjecting it to substitution with an amino group, a hydroxyl group or any other intended substituent at the 6-positioned halogen atom, nucleoside derivatives are produced at a high yield. Methods for producing nucleoside derivatives including 9-(2,3-dideoxy-2-fluoro-&bgr;-D-threo-pentofuranosyl)adenine (FddA) and their related compounds, in a simplified manner, at a high yield and at low costs, and especially Economical methods for substituting substrates, of which the 3′-position of the saccharide moiety is deoxylated, at the 2′-position to produce those nucleoside derivatives on an industrial scale are also provided.

    摘要翻译： 产生其核酸碱基部分的6位被卤素原子取代的核苷衍生物的新型中间体。 使用这些新型中间体，其中糖基部分的3'-位脱氧的偶联底物可以在2'-位以非常高的收率被取代。 具体来说，通过使肌苷的3'-脱氧衍生物进行6-卤化，得到该衍生物的6-卤化物，然后用氟原子等进行2'-脱氧/取代，然后进一步对其进行 以6-取代的卤素原子被氨基，羟基或任何其它目的取代基取代，以高产率生产核苷衍生物。 以简单的方式以高产率和低成本制备包括9-（2,3-二脱氧-2-氟-β-D-苏 - 呋喃鸟糖基）腺嘌呤（FddA）及其相关化合物的核苷衍生物的方法， 并且还提供了用于将2'-位上的糖部分的3'-位脱氧的底物替代为工业规模生产这些核苷衍生物的经济方法。

    Process for producing optically active 2-hydroxy-4-arylbutyric acid or its ester
    65.
    发明授权
    Process for producing optically active 2-hydroxy-4-arylbutyric acid or its ester 失效
    光学活性2-羟基-4-芳基丁酸或其酯的制备方法

    公开(公告)号：US06258975B1

    公开(公告)日：2001-07-10

    申请号：US09477740

    申请日：2000-01-05

    申请人： Masahiko Kurauchi ,  Yoshimasa Hagiwara ,  Hiroyuki Matsueda ,  Takashi Nakano ,  Kunisuke Izawa

    发明人： Masahiko Kurauchi ,  Yoshimasa Hagiwara ,  Hiroyuki Matsueda ,  Takashi Nakano ,  Kunisuke Izawa

    IPC分类号： C07C6976

    CPC分类号： C07C69/732 ,  C07C51/377 ,  C07C67/317 ,  C07C67/343 ,  C07C59/48 ,  C07C69/738

    摘要： Provided is an industrially useful process for producing an optically active 2-hydroxy-4-arylbutyric acid or its ester. An optically active acyloxysuccinic anhydride is reacted with an aromatic compound in the presence of a Lewis acid to produce an optically active 2-acyloxy-4-oxo-4-arylbutyric acid. The 2-acyloxy-4-oxo-4-arylbutyric acid is converted to an optically active 2-acyloxy-4-arylbutyric acid through catalytic reduction. The 2-acyloxy-4-arylbutyric acid is hydrolyzed in the presence of an acid or an alkali to produce an optically active 2-hydroxy-4-arylbutyric acid. The 2-hydroxy-4-arylbutyric acid is reacted with an alcohol in the presence of an acid to produce an optically active 2-hydroxy-4-arylbutyric acid ester.

    摘要翻译： 提供了用于制备光学活性2-羟基-4-芳基丁酸或其酯的工业上有用的方法。 在路易斯酸存在下，使光学活性的酰氧基琥珀酸酐与芳族化合物反应，得到光学活性的2-酰氧基-4-氧代-4-芳基丁酸。 通过催化还原将2-酰氧基-4-氧代-4-芳基丁酸转化成光学活性的2-酰氧基-4-芳基丁酸。 2-酰氧基-4-芳基丁酸在酸或碱的存在下水解，得到光学活性的2-羟基-4-芳基丁酸。 2-羟基-4-芳基丁酸与醇在酸的存在下与醇反应，得到光学活性的2-羟基-4-芳基丁酸酯。

    Process for producing propionic acid derivatives
    66.
    发明授权
    Process for producing propionic acid derivatives 失效
    丙酸衍生物的制备方法

    公开(公告)号：US06242635B1

    公开(公告)日：2001-06-05

    申请号：US09156900

    申请日：1998-09-18

    申请人： Takayuki Suzuki ,  Takayuki Hamada ,  Kunisuke Izawa

    发明人： Takayuki Suzuki ,  Takayuki Hamada ,  Kunisuke Izawa

    IPC分类号： C07C6700

    CPC分类号： C07C67/333 ,  C07C51/09 ,  C07C51/36 ,  C07C51/367 ,  C07C67/303 ,  C07C67/31 ,  C07C67/343 ,  C07C59/48 ,  C07C69/732

    摘要： A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.

    摘要翻译： 一种2-芳烷基-3-羟基丙酸（或其酯）的制备方法，包括以下步骤：将通过芳基醛反应容易得到的3-羟基-2-亚甲基-3-芳基丙酸酯与 丙烯酸酯与酸酐反应形成2-芳烷叉-3-酰氧基丙酸酯; 使其同时进行水解或醇解; 并减少所得2-亚烷基-3-羟基丙酸或其酯。 还原步骤可以在碱的存在下进行。

    Method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids
    67.
    发明授权
    Method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids 失效

    公开(公告)号：US06239308B1

    公开(公告)日：2001-05-29

    申请号：US09679283

    申请日：2000-10-06

    申请人： Takayuki Suzuki ,  Yutaka Honda ,  Kunisuke Izawa

    发明人： Takayuki Suzuki ,  Yutaka Honda ,  Kunisuke Izawa

    IPC分类号： C07C32100

    CPC分类号： C07C323/29 ,  C07C317/28 ,  C07C327/30

    摘要： The present invention provides a simple and inexpensive method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids and their esters. An ester of an N-protected &agr;-amino acid ester is converted into a &bgr;-ketosulfoxide, which is then processed with an acid to give an &agr;-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected &agr;-acyloxy-&bgr;-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce &agr;-hydroxy-&bgr;-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.

    Optically active pyrrolidine derivative
    68.
    发明授权
    Optically active pyrrolidine derivative 失效
    光学活性吡咯烷衍生物

    公开(公告)号：US5342963A

    公开(公告)日：1994-08-30

    申请号：US915808

    申请日：1992-09-15

    申请人： Kuniya Sakurai ,  Kunisuke Izawa ,  Hiroyuki Izawa ,  Takashi Ineyama ,  Tomihisa Ohta ,  Shigeo Nozoe

    发明人： Kuniya Sakurai ,  Kunisuke Izawa ,  Hiroyuki Izawa ,  Takashi Ineyama ,  Tomihisa Ohta ,  Shigeo Nozoe

    IPC分类号： C07D207/16 ,  C07D401/06 ,  C07D477/02 ,  C07D477/04 ,  C07D477/14 ,  C07D477/20 ,  C07D207/00 ,  C07D401/00 ,  C07D405/00 ,  C07D487/00

    CPC分类号： C07D477/20 ,  C07D207/16 ,  C07D401/06 ,  C07D477/02 ,  C07D477/04 ,  C07D477/14 ,  Y02P20/55

    摘要： Optically active pyrrolidine derivative represented by the following formula (XI): ##STR1## wherein R.sup.1 represents a benzyl group R.sup.2 represents an alkyl group having 1 to 6 carbon atoms, R.sup.3 represents an alkyl group having 1 to 6 carbon atoms, a benzyl group or an allyl group, R.sup.4 is selected from the group consisting of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms which may be substituted with a protected hydroxyl group, a vinyl group, a phenyl group which may be substituted, a benzyl group which may be substituted, and a heterocyclic ring having 1 to 4 nitrogen or/and oxygen atoms, and R.sup.5 represents a hydrogen atom or a methyl group.This compound can be an intermediate for synthesis of carbapenem antibiotic compounds.

    摘要翻译： PCT No.PCT / JP91 / 01619 Sec。 371日期：1992年9月15日 102（e）日期1992年9月15日PCT 1991年11月26日PCT PCT。 出版物WO92 / 09605 日期：6月11日，1992。下式（XI）表示的视觉活性吡咯烷衍生物：其中R1表示苄基R2表示碳原子数1〜6的烷基，R3表示具有 1至6个碳原子，苄基或烯丙基，R 4选自氢原子，可被被保护的羟基取代的具有1至6个碳原子的烷基，乙烯基， 可以被取代的苯基，可以被取代的苄基，以及具有1〜4个氮原子或/或氧原子的杂环，R 5表示氢原子或甲基。 该化合物可以是合成碳青霉烯类抗生素化合物的中间体。

    Inosine derivatives and production methods therefor
    70.
    发明授权
    Inosine derivatives and production methods therefor 失效
    肌苷衍生物及其制备方法

    公开(公告)号：US08288526B2

    公开(公告)日：2012-10-16

    申请号：US12847399

    申请日：2010-07-30

    申请人： Takayoshi Torii ,  Kunisuke Izawa ,  Doo Ok Jang ,  Dae Hyan Cho

    发明人： Takayoshi Torii ,  Kunisuke Izawa ,  Doo Ok Jang ,  Dae Hyan Cho

    IPC分类号： C07H19/173 ,  C07H19/167 ,  C07H19/16

    CPC分类号： C07D473/30 ,  C07H19/167

    摘要： The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).

    摘要翻译： 本发明提供由以下通式（1）表示的肌苷衍生物的制造方法，其特征在于，包括使通式（3）的肌苷衍生物进行二硫代羰基化，进行所得化合物的自由基还原的工序。 根据本发明，可以生产用于工业规模的抗艾滋病药物的化合物。 其中R 1可以相同或不同，并且各自可以在通式（1）和（3）中具有取代基的苄基，二苯甲基或三苯甲基。