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    2-(HYDROXYMETHYL) ACRYLATE DERIVATIVES AND PROCESS FOR THEIR PREPARATION
    2.
    发明申请
    2-(HYDROXYMETHYL) ACRYLATE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
    2-（羟甲基）丙烯酸酯衍生物及其制备方法

    公开(公告)号：WO1991018861A1

    公开(公告)日：1991-12-12

    申请号：PCT/AU1991000236

    申请日：1991-05-31

    申请人： COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ... ,  STRAUSS, Christopher, Roy ,  GALBRAITH, Michael, Neil ,  FAUX, Alan, Francis

    发明人： COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ...

    IPC分类号： C07C45/72

    CPC分类号： C07C255/15 ,  C07C45/72 ,  C07C45/75 ,  C07C51/367 ,  C07C67/343 ,  C07C205/43 ,  C07C231/12 ,  C07C253/30 ,  C07C69/732 ,  C07C255/16 ,  C07C59/52 ,  C07C49/24 ,  C07C47/263

    摘要： A process for the preparation of a compound of general formula (I) which comprises reacting a compound of general formula (II) with a carbonyl compound of the general formula (III): RR6CO, wherein Z represents an electron withdrawing group and R6 represents hydrogen, branched or straight-chained, substituted or unsubstituted C1-18 alkyl, substituted or unsubstituted C5-C12 cycloalkyl, aralkyl or alkaryl and R in formulae (I and III) represents hydrogen, substituted or unsubstituted C1-C8 alkyl, lower alkenyl (C1-C8), alk-(C1-C4)aryl, aralkyl(C1-C4) or aryl, or R together with R6 may form a cyclic ring and R5 in formulae (I and II) represents hydrogen, C1-C18 alkyl, cycloalkyl, aralkyl, alkaryl, aryl or a heterocyclic ring such as a furyl ring, said reaction being carried out in the presence of microwave radiation.

    摘要翻译： 一种制备通式（I）化合物的方法，其包括使通式（II）的化合物与通式（III）的羰基化合物反应：RR6CO，其中Z代表吸电子基团，R6代表氢 ，支链或直链的取代或未取代的C1-18烷基，取代或未取代的C5-C12环烷基，芳烷基或烷芳基，式（I和III）中的R代表氢，取代或未取代的C1-C8烷基，低级烯基（C1 -C（C 1 -C 6）烷基，C 1 -C 4芳基，芳烷基（C 1 -C 4）或芳基，或R 6与R 6一起形成环，式（I和II）中的R 5表示氢， ，芳烷基，烷芳基，芳基或杂环如呋喃基，所述反应在微波辐射存在下进行。

    PROCESS FOR PREPARING 4-CHLORO-3-HYDROXYBUTANOIC ACID ESTER
    9.
    发明申请
    PROCESS FOR PREPARING 4-CHLORO-3-HYDROXYBUTANOIC ACID ESTER 审中-公开
    制备4-氯-3-羟基丁酸的方法

    公开(公告)号：WO2004092114A1

    公开(公告)日：2004-10-28

    申请号：PCT/KR2004/000869

    申请日：2004-04-14

    申请人： LG LIFE SCIENCES LTD. ,  CHO, Sung-Wook ,  CHANG, Jay-Hyok ,  LEE, Kyu-Woong ,  LEE, Ki-Kon ,  SO, Byung-Ran ,  SHIN, Hyun-Ik

    发明人： CHO, Sung-Wook ,  CHANG, Jay-Hyok ,  LEE, Kyu-Woong ,  LEE, Ki-Kon ,  SO, Byung-Ran ,  SHIN, Hyun-Ik

    IPC分类号： C07C253/04

    CPC分类号： C07C253/00 ,  C07B2200/07 ,  C07C67/22 ,  C07C253/16 ,  C07C69/675 ,  C07C255/12 ,  C07C255/15

    摘要： The present invention relates to a process for preparing 4-chloro-3-hydroxybutanoic acid ester, an intermediate for preparing atorvastatin, in high purity and yield, by comprising the steps of 1) reacting epichlorohydrin of formula (2) with cyanide of formula (3) under the condition of pH ranging from 7 to 8, to form the 4-chloro-3-hydroxybutyronitrile of formula (4) and 2a) dissolving the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent and reacting it with hydrogen chloride, or 2b) reacting the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent saturated with hydrogen chloride, to form the 4-chloro-3-hydroxybutyronitrile acid ester of formula (I).

    摘要翻译： 本发明涉及一种制备4-氯-3-羟基丁酸酯的方法，该方法是高纯度和高收率制备阿托伐他汀的中间体，包括以下步骤：1）使式（2）的表氯醇与式（2）的氰化物反应， 3）在pH为7至8的条件下，形成式（4）的4-氯-3-羟基丁腈和2a）将式（4）的4-氯-3-羟基丁腈溶解在醇溶剂中， 使其与氯化氢反应，或2b）使式（4）的4-氯-3-羟基丁腈在饱和氯化氢的醇溶剂中反应，形成式（I）的4-氯-3-羟基丁腈酸酯。

    PROCESS FOR THE CYANATION OF ALDEHYDES
    10.
    发明申请
    PROCESS FOR THE CYANATION OF ALDEHYDES 审中-公开
    醛脱氢酶的方法

    公开(公告)号：WO02010095A3

    公开(公告)日：2002-04-18

    申请号：PCT/GB2001/003456

    申请日：2001-08-01

    IPC分类号： B01J31/22 ,  B01J31/18 ,  C07B53/00 ,  C07B61/00 ,  C07C253/00 ,  C07C255/14 ,  C07C255/15 ,  C07C255/38

    CPC分类号： B01J31/2243 ,  B01J2231/341 ,  B01J2531/0205 ,  B01J2531/0252 ,  B01J2531/46 ,  B01J2531/56 ,  C07B53/00 ,  C07C253/00 ,  C07C255/14 ,  C07C255/15 ,  C07C255/38

    摘要： A process for cyanating an aldehyde is provided. The process comprises reacting the aldehyde with: i) a cyanide source which does not comprise a Si-CN bond or a C-(C=O)-CN moiety; and ii) a substrate susceptible to nucleophilic attack not comprising a halogen leaving group; in the presence of a chiral catalyst. Preferably, the chiral catalyst is a chiral vanadium or titanium catalyst. The cyanide source is preferably an alkali metal cyanide and the substrate susceptible to nucleophilic attack not comprising a halogen leaving group is a carboxylic anhydride.

    摘要翻译： 提供了一种氰化醛的方法。 该方法包括使醛与：i）不包含Si-CN键或C-（C = O）-CN部分的氰化物源反应; 和ii）对不包含卤素离去基团的亲核攻击敏感的底物; 在手性催化剂的存在下。 优选地，手性催化剂是手性钒或钛催化剂。 氰化物源优选为碱金属氰化物，并且对不含卤素离去基团的亲核侵袭敏感的底物是羧酸酐。