PROCESS FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID SUBSTITUTED IN 2-POSITION
    12.
    发明公开
    PROCESS FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID SUBSTITUTED IN 2-POSITION 审中-公开
    VERFAHREN ZUR HERSTELLUNG OPTISCH在2-STELLUNG SUBSTITERERTERCARBONSÄUREN

    公开(公告)号:EP1251115A1

    公开(公告)日:2002-10-23

    申请号:EP01946842.0

    申请日:2001-01-25

    摘要: A nitrous acid salt is added at a temperature of 10 to 80°C to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).

    摘要翻译: 在10〜80℃的温度下向含有光学活性的2-氨基羧酸(4)和质子酸的水溶液中加入亚硝酸盐,后者酸的量相对于前者为1〜3当量 ,其质子浓度为0.5〜2mol / kg进行反应,由此制造光学活性的2-羟基羧酸(1)。 使亚硫酰氯和碱性化合物作用于化合物(1)以使其氯化,同时反转2-位的构型。 因此,引发光学活性的2-氯羧酰氯(5)。 将化合物(5)水解以诱导光学活性的2-氯羧酸(2)。 使化合物(2)与硫代乙酸盐反应以并入其中的乙酰硫基,同时反转2-位的构型,从而产生光学活性的2-乙酰基硫代羧酸(3)。

    METHOD FOR PRODUCING CHLOROFORMATE COMPOUND
    13.
    发明公开

    公开(公告)号:EP3489216A1

    公开(公告)日:2019-05-29

    申请号:EP17830897.9

    申请日:2017-07-11

    IPC分类号: C07C68/02 C07C69/96

    摘要: The present invention provides a method for safely producing a large amount of chloroformate compound with high yield. The chloroformate compound can be produced by mixing and reacting a solution of triphosgene ,an amine and an alcohol compound in a flow reactor. The chloroformate compound can also be produced by mixing and reacting a solution of triphosgene with a solution comprising an amine and an alcohol compound in a flow reactor. The amine is preferably tributylamine, and preferably used in an amount of 0.8 to 3 equivalents relative to an amount of the alcohol compound.

    METHOD FOR PRODUCING OPTICALLY ACTIVE HYDROXYCARBOXYLIC ACID DERIVATIVE OR SALT THEREOF
    14.
    发明公开
    METHOD FOR PRODUCING OPTICALLY ACTIVE HYDROXYCARBOXYLIC ACID DERIVATIVE OR SALT THEREOF 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVENHYDROXYCARBONSÄUREDERIVATSODER SALZES DAVON

    公开(公告)号:EP2053032A1

    公开(公告)日:2009-04-29

    申请号:EP07805906.0

    申请日:2007-08-08

    摘要: The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.

    摘要翻译: 本发明的目的是提供一种制备光学活性羟基羧酸衍生物的方法,该方法是生产药物,农用化学品,化学产品等的重要中间体。 本发明的制造方法包括:通过光学活性二胺配合物的反应进行酮羧酸或其盐的氢转移还原,制造光学活性羟基羧酸衍生物。 根据本发明,可以安全有效地制造工业上有用的光学活性羟基羧酸衍生物。

    METHOD OF PRODUCING PEPTIDE
    15.
    发明公开
    METHOD OF PRODUCING PEPTIDE 审中-公开
    用于生产肽

    公开(公告)号:EP1995254A1

    公开(公告)日:2008-11-26

    申请号:EP06782052.2

    申请日:2006-07-31

    IPC分类号: C07K1/02

    摘要: The present invention is related to a method of producing a peptide, characterized in contacting a reaction mixture with a base after a condensation reaction to hydrolyze while a basic condition is maintained until a ratio of a remaining unreacted active ester of an acid component is decreased to 1% or less in a liquid phase peptide synthesis method. According to the invention, a target peptide of high purity can be simply and efficiently produced by a continuous liquid phase synthesis method. Further, the present invention is related to a method of producing a peptide, characterized in using an amide-type solvent immiscible with water in a liquid phase peptide synthesis method. According to the invention, various peptides can be produced by the liquid phase synthesis method without being restricted by the amino acid sequence of the target peptide.

    OPTICALLY ACTIVE HALOHYDRIN DERIVATIVE AND PROCESS FOR PRODUCING OPTICALLY ACTIVE EPOXY ALCOHOL DERIVATIVE FROM THE SAME
    16.
    发明公开
    OPTICALLY ACTIVE HALOHYDRIN DERIVATIVE AND PROCESS FOR PRODUCING OPTICALLY ACTIVE EPOXY ALCOHOL DERIVATIVE FROM THE SAME 有权
    光有源卤代和工艺及其生产光学活性EPOXYALKOHOLDERIVATS

    公开(公告)号:EP1647551A1

    公开(公告)日:2006-04-19

    申请号:EP04747351.7

    申请日:2004-07-05

    摘要: The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxyalcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.

    摘要翻译: 本发明提供工业上上安全,易于操作处理,用于光学活性环氧醇衍生物可用作在中间从廉价地获得的材料制备药物,并且因此提供了一种新型的卤代醇在重要中间体衍生物用作用于环氧醇衍生物。 进一步地,本发明提供了用于通过允许卤代醇与三唑磺酰胺,该方法包括少量步骤反应在中间为三唑类抗真菌剂的制造方法。 一种用于在光学活性环氧醇衍生物的制造方法包括:允许向旋光±取代丙酸酯衍生物在碱的存在下,卤代乙酸衍生物反应来制备光学活性的卤代酮衍生物,使所得卤代酮衍生物与在反应 芳金属化合物立体选择性地制备卤代醇衍生物,消除了对卤代醇衍生物的羟基的取代基,并用碱进行环氧化作用。 进一步,在中间制造用于三唑类抗真菌剂的方法包括:允许卤代醇衍生物与三唑磺酰胺,该方法包括少量步骤反应。

    PROCESS FOR PRODUCING 6-CYANOMETHYL-1,3-DIOXANE-4-ACETIC ACID DERIVATIVES
    17.
    发明公开
    PROCESS FOR PRODUCING 6-CYANOMETHYL-1,3-DIOXANE-4-ACETIC ACID DERIVATIVES 有权
    生产6-氰基甲基-1,3-二氧戊环-4-乙酸衍生物的方法

    公开(公告)号:EP1077212A1

    公开(公告)日:2001-02-21

    申请号:EP99917207.5

    申请日:1999-04-28

    摘要: A process whereby 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, which are important intermediates of an HMG coenzyme A reductase atorvastatin, can be industrially, easily and efficiently produced. This process comprises starting with a 3,5-dihydroxy-6-halohexane derivative, treating it with a cyaniding agent to thereby substitute the halogen atom with the cyano group (i.e., a cyanation reaction) and forming an acetal of a diol by using an acetal-forming agent in the presence of an acid catalyst (i.e., an acetal-formation reaction).

    摘要翻译: 作为HMG辅酶A还原酶阿托伐他汀的重要中间体的6-氰基甲基-1,3-二恶烷-4-乙酸衍生物的工艺可以在工业上,容易和有效地生产。 该方法包括从3,5-二羟基-6-卤代己烷衍生物开始,用氰化剂处理它,从而用氰基取代卤素原子(即氰化反应),并通过使用一种二醇形成二醇的缩醛 在酸催化剂存在下缩醛形成剂(即缩醛形成反应)。