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    PRODUCTION OF 1,2,4-THIAZIAZOLE-5-THIOL OR SALT THEREOF
    1.
    发明专利
    PRODUCTION OF 1,2,4-THIAZIAZOLE-5-THIOL OR SALT THEREOF 失效

    公开(公告)号：JPH01308270A

    公开(公告)日：1989-12-12

    申请号：JP13795688

    申请日：1988-06-03

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： MUKUDA TAKASHI ,  UEMATSU RYOICHI ,  HIRABAYASHI SATOSHI

    IPC: C07D285/08

    Abstract: PURPOSE:To obtain the title compound useful as a synthetic raw material for beta-lactam based antibiotic in one process, high yield and low cost, by reacting formamidine, or salt thereof with a xanthic acid O-ester and sulfur using the above-mentioned compounds as raw materials. CONSTITUTION:Formamidine or salt thereof is reacted with xanthic acid O-ester or salt thereof and sulfur normally in a solvent such as water, acetone or chloroform at ambient temperature or while heating to provide the aimed compound. The xanthic acid O-ester includes O-alkylxanthic acid such as O-methylxanthic acid, especially preferably 1-6C alkylxanthic acid. Further, the xanthic acid O-ester and salt thereof can be readily synthesized from carbon disulfide and alcoholic base and can be reacted with formamidine after isolating or without isolating.

    PRODUCTION OF 4-ALKANOYL-2-HALOANILINE
    4.
    发明专利
    PRODUCTION OF 4-ALKANOYL-2-HALOANILINE 失效

    公开(公告)号：JPH04312559A

    公开(公告)日：1992-11-04

    申请号：JP10664491

    申请日：1991-04-10

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ZANKA ATSUHIKO ,  HIRABAYASHI SATOSHI ,  MUKUDA TAKASHI ,  KUBOTA ARIKATSU

    IPC: C07C221/00 ,  C07C225/22

    Abstract: PURPOSE:To industrially and advantageously obtain 4-alkanoyl-2-haloanilines useful as an intermediate for alkanesulfonanilide derivatives having pharmacological actions such as anti-inflammatory and analgesic actions by using a stable halogenating reagent. CONSTITUTION:A 4-alkanoylaniline or its salt is reacted with an N- halosuccinimide stable to heat, shock, etc., in the presence of an aromatic amine according to a conventional method to selectively halogenate the 2-position of the 4-alkanoylaniline. Thereby, the objective 4-alkanoyl-2-haloaniline or its salt is industrially and advantageously obtained.

    PRODUCTION OF L-ARGININE
    5.
    发明专利
    PRODUCTION OF L-ARGININE 失效

    公开(公告)号：JP2000080072A

    公开(公告)日：2000-03-21

    申请号：JP18860599

    申请日：1999-07-02

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： MUKAI KOJI ,  MUKUDA TAKASHI ,  KAWAKAMI RYOICHI

    IPC: C07C277/08 ,  C07C279/14

    Abstract: PROBLEM TO BE SOLVED: To obtain L-arginine having a small crystal particle size distribution width in good particle size distribution repeatability and suitable for powder filling treatments by adding a specific amount of L-arginine crystals as seed crystals to a supersaturated solution of the L-arginine, when the L-arginine is crystallized. SOLUTION: This method for producing arginine crystals comprises crystallizing L-arginine. Therein, L-arginine crystals are added as seed crystals to the supersaturated solution of the L-arginine. The L-arginine crystals use for the seed crystals are preferably particulate L-arginine which has an average particle diameter of 100-300 μm and to which many fine L-arginine crystals (preferably fine L-arginine crystals having a particle diameter of 0.5-2 μm in an amount of 1×109 to 1×1011 crystals/g of the seed crystals) are preferably adhered as secondary nuclei used as the crystallization of the L-arginine. The L-arginine crystals used as the seed crystals may be fine L-arginine crystals obtained by grinding L-arginine crystals by the use of a grinder, etc., and having a particle diameter of 0.5-2 μm.

    PRODUCTION OF ALKANESULFONANILIDE DERIVATIVE
    7.
    发明专利
    PRODUCTION OF ALKANESULFONANILIDE DERIVATIVE 失效

    公开(公告)号：JPH051023A

    公开(公告)日：1993-01-08

    申请号：JP12218791

    申请日：1991-04-23

    Applicant: FUJISAWA PHARMACEUTICAL CO

    Inventor： ZANKA ATSUHIKO ,  MUKUDA TAKASHI ,  HIRABAYASHI SATOSHI

    IPC: C07C303/38 ,  A61K31/18 ,  C07C20060101 ,  C07C43/257 ,  C07C303/40 ,  C07C311/08 ,  C07C311/09 ,  C07C319/06 ,  C07C319/18 ,  C07C323/09 ,  C07C323/37 ,  C07C323/49 ,  C07C323/63

    Abstract: PURPOSE:To produce an alkanesulfoneanilide derivative or salt thereof having antiphlogistic action and analgesic action from a new raw material, in reduced producing processes and good yield. CONSTITUTION:A new compound expressed by formula I (R is lower alkyl; R is CN, CONH2 or lower alkanoyl; X is halogen) or salt thereof is reacted with a compound expressed by formula II (R and R are halogen; A is O or S; M is H, alkali metal or Cu) or salt thereof in the presence of a copper-base catalyst and a base using an aromatic amine based solvent to directly provide a compound expressed by formula III or salt thereof in high yield without using a preliminary process required in a conventional method. Furthermore, the new above-mentioned raw material can be produced by reacting a compound expressed by formula IV, its reactive derivative of the amino group or salt thereof with a compound expressed by the formula R SO2OH, its reactive derivative of the sulfonic acid group or salt thereof to give a compound expressed by formula V or salt thereof and then hologenating the compound expressed by formula V or salt thereof.

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