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    PRODUCTION OF THIAZOLYLBENZOFURAN DERIVATIVE
    3.
    发明专利
    PRODUCTION OF THIAZOLYLBENZOFURAN DERIVATIVE 失效

    公开(公告)号：JPH10316678A

    公开(公告)日：1998-12-02

    申请号：JP12739697

    申请日：1997-05-16

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： NISHIWAKI MASANORI ,  ZANKA ATSUHIKO ,  KUBOTA ARIKATSU ,  GOSHIMA SHUNSUKE

    IPC: C07D417/04 ,  A61K31/425 ,  A61P37/08 ,  A61P43/00

    Abstract: PROBLEM TO BE SOLVED: To efficiently produce the subject compound useful as a slow reacting substance antagonist or an inhibitor, of leukotriene/anaphylaxisin by one process. SOLUTION: A compound of formula I (R is a halogen, a lower alkylamino, etc.; R is H, a halogen, etc.; R is H, a halogen, a hydroxy, a lower alkyl, etc.; Y is O or S) or a pharmaceutically acceptable salt thereof is reacted with a compound of formula II (A is a lower alkylene; X is a single bond or a lower alkylene) thereof in the presence of a base to provide the objective thiazolylbenzofuran derivative of formula III or a pharmaceutically acceptable salt thereof in good yield by only one process. For instance, 4-tert-butyl-2-[5-(2- carboxymethylphenylmethoxy)benzofuran-2-yl)thiazole is obtained by reacting 4-tert-butyl-2-(5-hydroxybenzofuran-2-yl)thiazole with 3-isochromanon.

    ANTHRANILIC ACID DERIVATIVE
    6.
    发明专利
    ANTHRANILIC ACID DERIVATIVE 失效

    公开(公告)号：JPH0558974A

    公开(公告)日：1993-03-09

    申请号：JP29855491

    申请日：1991-08-27

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： KAGARA KOUJI ,  GOSHIMA SHUNSUKE ,  KODERA TETSUO ,  TSUBOI HIROYUKI

    IPC: C07C227/06 ,  C07C229/56

    Abstract: PURPOSE:To safely and easily obtain the subject compound useful as a raw material for quinazoline derivatives and medicines at low cost and in high yield by reducing a nitrobenzoic acid derivative. CONSTITUTION:The objective compound of formula II can be obtained by reacting a compound of formula I (R is H, halogen or lower alkoxy) or its salt with a reducing agent (e.g. hydrazine) in the presence of a catalyst (e.g. ferric chloride-activated carbon) in a solvent (e.g. isopropyl alcohol) at room temperature to higher temperatures. The compound of the formula I can be prepared by oxidation of a compound of formula III.

    PRODUCTION OF PYRIMIDINONE COMPOUND
    8.
    发明专利
    PRODUCTION OF PYRIMIDINONE COMPOUND 失效

    公开(公告)号：JPH02256669A

    公开(公告)日：1990-10-17

    申请号：JP34211489

    申请日：1989-12-27

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： KAGARA KOUJI ,  GOSHIMA SHUNSUKE ,  TSUBOI HIROYUKI

    IPC: C07D239/47

    Abstract: PURPOSE:To obtain the subject substance in a simple process by reacting 6-(3,4- dimethoxyphenyl)-3-methyl-2,4(1H,3H)-pyrimidinedione, etc., with 2,4,6- trimethylaniline, etc., in the presence of a reagent for activating oxo groups. CONSTITUTION:A compound expressed by formula I (R and R are H or lower alkyl; R is aryl which may have a substituent group) is reacted with a compound expressed by formula II (R is aryl which may have a substituent group) or salt thereof in the presence of a reagent (e.g. PCl3, P2O5, thionyl chloride or phosgene) capable of activating oxo groups of the compound expressed by formula I to afford a compound expressed by formula III. The compound, expressed by formula III and having cardiotonic action, etc., can be readily obtained in high yield for a short time according to the above-mentioned method without using H2S, alkyl halides, etc., which are toxic substances and considered as industrially undesirable.

    PRODUCTION OF QUINAZOLINE DERIVATIVE OR SALT THEREOF
    9.
    发明专利
    PRODUCTION OF QUINAZOLINE DERIVATIVE OR SALT THEREOF 失效

    公开(公告)号：JPS6425767A

    公开(公告)日：1989-01-27

    申请号：JP7562388

    申请日：1988-03-28

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： KAGARA KOUJI ,  GOSHIMA SHUNSUKE ,  TSUBOI HIROYUKI

    IPC: C07F7/10 ,  C07D239/96

    Abstract: PURPOSE:To easily and safely obtain the titled compound useful as a synthetic intermediate for anti-inflammatory agent or a synthetic intermediate for a drug for the remedy of complications of diabetes, in high yield at a low cost, by reacting a specific compound with a silylation agent and then a compound such as ethyl bromoacetate. CONSTITUTION:The objective compound of formula III can be produced by (1) reacting a compound of formula I (R is H or halogen) or its salt with a silylation agent [e.g. hexamethyldisilazane, trimethylchlorosilane or N,O-bis(trimethylsilyl)acetamide] in a solvent such as toluene usually under cooling or at room temperature, (2) reacting the product with a compound of formula II [R is alkyl, lower alkenyl, lower aralkyl or R -Z (R is carboxyl; Z is lower alkylene); X is acid residue] or its salt and, as necessary, (3) desilylating the reaction product. The desilylation is carried out by hydrolysis, alcoholysis, etc.

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