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    INTERMEDIATE OF ERIBULIN, SYNTHESIS METHOD THEREFOR AND USE THEREOF
    1.
    发明公开
    INTERMEDIATE OF ERIBULIN, SYNTHESIS METHOD THEREFOR AND USE THEREOF 审中-公开

    公开(公告)号：EP3925948A1

    公开(公告)日：2021-12-22

    申请号：EP20796052.7

    申请日：2020-04-02

    申请人： Beijing Tienyi Lufu Pharmatech Co. Ltd.

    发明人： XU, Weiping

    IPC分类号： C07C43/23 ,  C07C41/26 ,  C07D303/04 ,  C07D301/24 ,  C07D317/22 ,  C07D407/06 ,  C07F7/08 ,  C07F7/18

    摘要： The present invention relates to the field of drug synthesis, and particularly relates to an intermediate of eribulin and a synthesis method and use thereof. The present invention provides an intermediate useful for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof, and a preparation method and use thereof. The starting materials of the synthetic route disclosed herein are cheap and easy to obtain, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured; steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV); by-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.

    Conversion of a multihydroxylated aliphatic hydrocarbon or ester thereof to a chlorohydrin
    4.
    发明公开
    Conversion of a multihydroxylated aliphatic hydrocarbon or ester thereof to a chlorohydrin 有权
    多羟基脂族烃或其酯转化成氯代醇

    公开(公告)号：EP2181979A1

    公开(公告)日：2010-05-05

    申请号：EP09177404.2

    申请日：2005-07-18

    申请人： DOW GLOBAL TECHNOLOGIES INC.

    发明人： Schreck, David J. ,  Kruper, William, J. Jr. ,  Varjian, Richard D. ,  Jones, Mark E. ,  Campbell, Robert M. ,  Kearns, Kenneth Jr. ,  Hook, Bruce D. ,  Briggs, John R. ,  Hippler, Jeffrey G.

    IPC分类号： C07C29/62 ,  C07D303/08 ,  C07D301/24

    CPC分类号： C07D301/24 ,  C07C29/62 ,  C07C29/82 ,  C07C31/36 ,  C07C31/42

    摘要： A process for converting a multihydroxylated-aliphatic hydrocarbon or ester thereof to a chlorohydrin, by contacting the multihydroxylated-aliphatic hydrocarbon or ester thereof starting material with a source of a superatmospheric partial pressure of hydrogen chloride for a sufficient time and at a sufficient temperature, and wherein such contracting step is carried out without substantial removal of water, to produce the desired chlorohydrin product; wherein the desired product or products can be made in high yield without substantial formation of undesired overchlorinated byproducts. In addition, certain catalysts of the present invention may be used in the present process at superatmospheric, atmospheric and subatmospheric pressure conditions with improved results.

    摘要翻译： 通过使多羟基化脂族烃或其酯与起始材料与超大气压氯化氢分压源接触足够的时间并在足够的温度下将多羟基化脂族烃或其酯转化为氯代醇的方法，以及 其中这种收缩步骤是在基本上不除去水的情况下进行的，以产生所需的氯代醇产物; 其中可以高收率地制备所需的一种或多种产物而基本不会形成不希望的过氯化副产物。 另外，本发明的某些催化剂可以在超大气压，大气压和低于大气压条件下用于本发明方法中，并具有改进的结果。

    FLUORINE-CONTAINING ADAMANTANE DERIVATIVE, FLUORINE-CONTAINING ADAMANTANE DERIVATIVE HAVING POLYMERIZABLE GROUP, RESIN COMPOSITION CONTAINING THE SAME, AND ANTIREFLECTION FILM
    5.
    发明公开
    FLUORINE-CONTAINING ADAMANTANE DERIVATIVE, FLUORINE-CONTAINING ADAMANTANE DERIVATIVE HAVING POLYMERIZABLE GROUP, RESIN COMPOSITION CONTAINING THE SAME, AND ANTIREFLECTION FILM 审中-公开
    FLUOR含金刚烷，福陆含金刚烷聚合的基团，树脂组合物这包含和防反射膜

    公开(公告)号：EP2014639A1

    公开(公告)日：2009-01-14

    申请号：EP07742063.6

    申请日：2007-04-20

    申请人： Idemitsu Kosan Co., Ltd.

    发明人： OKADA, Yasunari ,  YAMANE, Hideki ,  ITO, Hajime ,  MATSUMOTO, Nobuaki

    IPC分类号： C07C69/653 ,  C07C31/44 ,  C07C67/14 ,  C07D301/24 ,  C07D303/30 ,  C08L101/00 ,  G02B1/04 ,  G02B1/11

    CPC分类号： C07C31/44 ,  C07C69/653 ,  C07C2603/74 ,  C07D301/24 ,  C07D305/06 ,  C08F220/24 ,  C08F222/1006

    摘要： To provide a polymerizable group-containing and fluorine-containing adamantane derivative capable of affording a cured product having good heat resistance, good mechanical properties such as mar resistance and a low refractive index, a resin composition containing such a polymerizable group-containing adamantane derivative, and a fluorine-containing adamantane derivative which is useful as a reaction intermediate used for the production of the polymerizable group-containing and fluorine-containing adamantane derivative.
    Specifically provided are a fluorine-containing adamantane derivative represented by the general formula (I) below, a polymerizable group-containing and fluorine-containing adamantane derivative represented by the general formula (II) below, and a resin composition containing such a polymerizable group-containing and fluorine-containing adamantane derivative. In the formula, R 1 and R 2 are each a hydrogen atom, for example, n is an integer of 0 or more, X 1 is a polymerizable group represented by the formula (III-a), for example, Y is a hydrogen atom, for example, s and t are each an integer of 1 to 15, and u is an integer of 0 to 14, with the proviso that s + t + u = 16.

    摘要翻译： 提供和含氟金刚烷衍生物能够得到具有良好耐热性的固化物的含有聚合性基团的，良好的机械性能：如耐擦伤性和低折射率，含寻求含聚合性基团的金刚烷衍生物的树脂组合物， 和含氟金刚烷衍生物所有作为中间体的反应用于生产含聚合性基团的含氟金刚烷衍生物的，这是有用。 下面具体地提供了由通式（I）表示的含氟金刚烷衍生物，含有聚合性基团和由下面的通式（II）表示的含氟金刚烷衍生物，和树脂组合物包含寻求可聚合基团 - 含有氟和含金刚烷衍生物。 氢在该式中，R 1和R 2各自为氢原子，对于实施例中，n是0以上的整数，X 1是由式（III-A）表示的聚合性基团，例如，Y是 核，例如，s和t各自为1至15的整数，u是0〜14的整数，前提条件做S + T + U = 16

    VERFAHREN ZUR HERSTELLUNG VON OPTISCH AKTIVEN, PROPARGYLISCHEN, TERMINALEN EPOXIDEN
    6.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON OPTISCH AKTIVEN, PROPARGYLISCHEN, TERMINALEN EPOXIDEN 审中-公开
    用于生产光学活性的，丙炔，环氧化物终端

    公开(公告)号：EP1358173A1

    公开(公告)日：2003-11-05

    申请号：EP02706661.2

    申请日：2002-02-02

    申请人： FORSCHUNGSZENTRUM JÜLICH GMBH

    发明人： SCHUBERT, Thomas, A. ,  HUMMEL, Werner ,  MÜLLER, Michael

    IPC分类号： C07D301/24 ,  C07D303/02 ,  C12P17/02

    CPC分类号： C07D303/22 ,  C07B2200/07 ,  C07D303/04 ,  C07D303/08 ,  C07D303/40 ,  C07D409/06 ,  C07F7/083 ,  C12P7/02

    摘要： The invention relates to a method for enantioselective representation of optically active, propargylic, terminal epoxides. According to the invention, in a first step of the inventive method, compounds of formula I are reacted with an alcoholdehydrogenase which preferably originates from horse liver or thermophilic microorganisms (e.g. thermoanaerobium brockii or thermoanaerobacter ethanolicus) or from Lactobacillus and is recombinantly overexpressed in Escherichia coli, in the presence of NAD (P) H. During said reaction, the oxogroup is enantioselectively reduced. Since (S) selective and (R) selective oxidoreductases can be used, the synthesis of both enantiomers is possible. Representation of both enantiomers using the same enzyme is achieved with alkoholdehydrogenase from Lactobacillus brevis, since said compounds react with R1 = H and compounds with R1 = H to form alcohols having an opposite configuration. In the second step of the method, the α-halogenated alcohol is transformed into an enantiomer pure epoxide by means of a base.

    Process for manufacturing an epoxide
    9.
    发明公开
    Process for manufacturing an epoxide 审中-公开
    Herstellungsverfahrenfürein Epoxid

    公开(公告)号：EP2669307A1

    公开(公告)日：2013-12-04

    申请号：EP12170576.8

    申请日：2012-06-01

    申请人： SOLVAY SA

    发明人： Delannoy, Vincent

    IPC分类号： C08G59/04 ,  C08G59/06 ,  C08G59/02 ,  C07D301/24

    CPC分类号： C07D301/24 ,  C08G59/022 ,  C08G59/04 ,  C08G59/06 ,  C08G59/063

    摘要： Process for manufacturing an epoxide, comprising consuming a first compound containing chlorine (A), generating a second compound containing chlorine (B), converting (B) into (A), and wherein the molar ratio between consumed (A) and (A) converted from (B), expressed as elemental chlorine (Cl), is higher than or equal to 0.9.

    摘要翻译： 制备环氧化物的方法，包括消耗含有氯（A）的第一化合物，产生含氯的第二化合物（B），将（B）转化为（A），并且其中消耗的（A）和（A） 由（B）转化为元素氯（Cl）表示，高于或等于0.9。