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    PRODUCTION OF 6HYDROXY-2NAPHTHALDEHYDE AND RELATING COMPOUNDS
    3.
    发明专利
    PRODUCTION OF 6HYDROXY-2NAPHTHALDEHYDE AND RELATING COMPOUNDS 失效

    公开(公告)号：JPH10265427A

    公开(公告)日：1998-10-06

    申请号：JP6819597

    申请日：1997-03-21

    申请人： SUMIKIN CHEM KK

    发明人： TAKEDA KYOICHI ,  SATO TOSHIO

    IPC分类号： C07C45/43 ,  C07C47/36 ,  C07C67/29 ,  C07C67/307 ,  C07C69/157

    摘要： PROBLEM TO BE SOLVED: To produce 6hydroxy and 6-acyloxy-2-naphthoaldehyde inexpensively in high yield. SOLUTION: 2-Methyl-6naphthol is acetylated with acetic anhydride, the formed 6-acetyloxy-4naphthalene is allowed to react with a halogenating agent to form 6acetyloxy-2dihalogenomethylnaphthalene as an intermediate. This intermediate is hydrolyzed in the presence of hydrogen halide acid in a water- lower carboxylic acid mixed solvent to form 6-hydroxy-2-naphthoaldehyde, while is hydrolyzed in the presence of a lower carboxylic alkali salt in an amount of more than the equimolar amount to the halogen group in the intermediate to form 6-acetyloxy-2-naphthoaldehyde selectively in high yields in both cases.

    ANTITUMOR AGENT
    5.
    发明专利
    ANTITUMOR AGENT 失效

    公开(公告)号：JPS6434913A

    公开(公告)日：1989-02-06

    申请号：JP19016687

    申请日：1987-07-31

    申请人： MITSUBISHI CHEM IND

    发明人： NISHINO CHIKAO ,  KOBAYASHI KOJI ,  TAMAO YOSHIKUNI ,  OYA JUNICHI

    IPC分类号： A61K31/05 ,  A61K31/047 ,  A61K31/085 ,  A61K31/11 ,  A61K31/60 ,  A61P35/00 ,  C07C39/11 ,  C07C43/23 ,  C07C47/36 ,  C07C47/37 ,  C07C65/05 ,  C07C65/21

    摘要： PURPOSE:To provide an antitumor agent containing compounds existing in sumac of Rhus family as active components and exhibiting excellent action to inhibit the proliferation of Hela cell. CONSTITUTION:The compound of formula (X is hydroxy or methoxy; Y is carboxyl, aldehyde, hydroxymethyl or methoxycarbonyl; R is 15-17C alkyl; when X is methoxy, Y is carboxyl or hydroxymethyl) existing in the leaf of sumac (a plant of Rhus family) is used as an active component and prepared in the form of a drug by conventional method using conventional drug carrier to obtain the objective agent. It can be used in the form of injection, instillation, capsule, etc., and the rate of administration of the compound to adult is 5-100 mg/kg-body weight for injection and 20-500mg/kg-body weight for oral administration. The compound of formula can be produced by cutting leaves of sumac into small pieces, extracting with a proper solvent and purifying the extract by column chromatography.

    Preparation of bicyclo 3.3.0 octane derivative
    7.
    发明专利
    Preparation of bicyclo 3.3.0 octane derivative 失效
    BICYCLO 3.3.0 OCT衍生物的制备

    公开(公告)号：JPS5748933A

    公开(公告)日：1982-03-20

    申请号：JP12480380

    申请日：1980-09-09

    申请人： Sankyo Co Ltd

    发明人： AMAMIYA SHIGEO ,  KOJIMA KOUICHI ,  SAKAI KIYOSHI

    IPC分类号： C07D317/72 ,  C07C45/00 ,  C07C45/61 ,  C07C47/36 ,  C07C47/37 ,  C07C49/523 ,  C07C67/00

    CPC分类号： Y02P20/55

    摘要： PURPOSE: To prepare the titled compound useful as a synthetic intermediate of 9(O)-methanoprostacycline, etc., in a shortened production process, by the condensation reaction of diformylmethylcyclopentane derivative in the presence of a base or a base and a metal salt.
    CONSTITUTION: The objective compound of formula II such as 3α-hydroxy-4β- formvl-7-oxobicyclo[3.3.0]octane, etc. is prepared by the condensation reaction of the compound of formula I (A is oxo or carbonyl-protecting group) such as 1-oxo- 3α,4α-diformyl-methylcyclopentane in a solvent such as acetonitrile in the presence of a base such as pyridine hydrochloride or a combination of the base and a metal salt such as zinc acetate, in an inert gas tream (e.g. N
    2 ) at -10°C W about room temp. for 30minW10hr. The amount of by-product can be reduced by using a metal salt in combination with the base.
    USE: A synthetic intermediate of 9(O)methanoprostacycline or its derivative effective as a remedy and preventive for thermobosis.
    COPYRIGHT: (C)1982,JPO&Japio

    摘要翻译： 目的：通过二甲酰基甲基环戊烷衍生物在碱或碱和金属盐的存在下的缩合反应，缩短制备方法，制备作为9（O） - 甲醛前列环素等合成中间体的标题化合物。 构成：通过式I化合物（A是氧代或羰基保护基）的缩合反应制备式II的目标化合物，例如3α-羟基-4,4a-甲基-7-氧代双环[3.3.0]辛烷等 基团）如1-氧代-3α，4α-二甲酰基 - 甲基环戊烷在溶剂如乙腈中，在碱如吡啶盐酸盐或碱和金属盐如乙酸锌的组合的存在下，在惰性气体中 在-10摄氏度（例如N2） - 约室温 30min-10hr。 通过使用与碱组合的金属盐可以减少副产物的量。 用途：9（O）甲基前列腺素或其衍生物的合成中间体作为治疗和预防热病的有效方法。

    アルドール反応触媒
    8.
    发明专利
    アルドール反応触媒 审中-公开
    醛醇缩合反应的催化剂

    公开(公告)号：JPWO2014203944A1

    公开(公告)日：2017-02-23

    申请号：JP2015522965

    申请日：2014-06-18

    申请人： 国立大学法人京都大学

    发明人： 巧 古田 ,  智明 馬場 ,  猛夫 川端

    IPC分类号： B01J31/02 ,  C07C45/65 ,  C07C47/36

    CPC分类号： C07C45/72 ,  B01J31/1805 ,  B01J2231/342 ,  B01J2531/0266 ,  C07C311/09 ,  C07C311/21 ,  C07D207/12 ,  C07D211/42 ,  C07C47/36

    摘要： 本発明は、アルドール反応触媒およびこの触媒を用いた、立体選択的環状βヒドロキシアルデヒド化合物の製造方法を提供することを課題とする。斯かる課題を解決するための手段として、一般式(I):[化1][式中、R1、R2、R3a、R4a、Ra、Rは、明細書中に定義されるとおりである。]で表されるビアリール型アルドール反応触媒を提供する。

    摘要翻译： 本发明是用于醛醇缩合反应的催化剂和催化剂，以及提供用于制造立体选择性环状β羟基醛化合物的方法。 作为解决这种问题的手段，在通式（I）：[化学式1]其中，R1，R2中，R 3a中，R 4a中，R a，R如说明书中所定义。 提供由表示的联芳基类醛醇缩合反应的催化剂。