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    PRODUCTION OF AMIDES
    4.
    发明专利
    PRODUCTION OF AMIDES 失效

    公开(公告)号：JP2000095741A

    公开(公告)日：2000-04-04

    申请号：JP27139698

    申请日：1998-09-25

    Applicant: SUMITOMO CHEMICAL CO

    Inventor： NOYORI RYOJI ,  IWAKURA KAZUNORI ,  ODA YOSHIAKI

    IPC: B01J31/12 ,  C07B61/00 ,  C07C231/02 ,  C07C233/04 ,  C07C233/09 ,  C07C233/11 ,  C07C235/06 ,  C07C235/34 ,  C07C253/30 ,  C07C255/19

    Abstract: PROBLEM TO BE SOLVED: To obtain an amide in a high yield by reacting esters with amines in the presence of a specific organic tin compound. SOLUTION: The objective compound of formula III is obtained by reacting (A) esters of formula I [R1-R3 are each H, a halogen, cyano or the like; R4 is a (substituted) alkyl or the like] (e.g. 2-methyl fuloropropanate acid) with (B) amines of the formula: R5-NH2 [R5 is H, a (substituted) 6-20C aryl or the like] (e.g. 1phenylethylamine) in the presence of (C) an organic tin compound of formula II (X, Y and Z are each a 1-10C alkoxyl, alkylthio, a halogen or the like; R6 is H or a 1-3C alkyl; R7 is a 2-4C alkylene chain), e.g. 3- aminopropyltin triisopropoxide, preferably at 20-200 deg.C. Preferably, the component C in an amount of 0.001-200 mol % to the component A and the component B in the amount of 1 equivalent to the component A are respectively used in the reaction.

    NOVEL PRODUCTION METHOD OF BENZOIC ACID DERIVATIVE
    5.
    发明专利
    NOVEL PRODUCTION METHOD OF BENZOIC ACID DERIVATIVE 失效

    公开(公告)号：JP2000034262A

    公开(公告)日：2000-02-02

    申请号：JP20371799

    申请日：1999-07-16

    Applicant: SHUDO KOICHI

    Inventor： HAMADA YOSHINORI ,  YAMADA ISAMU ,  KAMINAKA MASAO ,  SAKATA TERUO

    IPC: A61K31/00 ,  A61K9/127 ,  A61K31/165 ,  A61K31/196 ,  A61P3/00 ,  C07C231/12 ,  C07C231/14 ,  C07C231/24 ,  C07C233/04 ,  C07C233/07 ,  C07C233/11 ,  C07C233/65 ,  C07C235/84

    Abstract: PROBLEM TO BE SOLVED: To obtain a novel compound which is useful for obtaining a benzoic acid derivative comprising a specific bicyclic amide compound, having retinoid activity and useful as medicines. SOLUTION: This benzoic acid derivative is a compound expressed by formula I (R1 is a lower alkyl or an aryl; R2 and R7 are each H or a lower alkyl; R3 to R6 are each a lower alkyl), e.g. 1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6- acetaminonaphthalene. The compound of formula I is obtained by carrying out the Friedel-Crafts reaction using 1 mole of an acylated aniline derivative of formula II with preferably 1.5-2 mole of 1,4-dihalobutane derivative of formula III (X is a halogen) and preferably 1.5-2 mole of a Lewis acid (e.g. AlCl3, etc.), a protonic acid (e.g. sulfuric acid, etc.), etc., as a catalyst. As a solvent, a halogenated hydrocarbon is preferably used. It is preferable to carry out the reaction at temperatures ranging from a room temperature to a cooled temperature for 0.5-20 hours.

    ANTIMICROBIAL AND ANTIFOULING AGENT AND BROMOACETAMIDE DERIVATIVE
    10.
    发明专利
    ANTIMICROBIAL AND ANTIFOULING AGENT AND BROMOACETAMIDE DERIVATIVE 失效

    公开(公告)号：JPH10204046A

    公开(公告)日：1998-08-04

    申请号：JP1081897

    申请日：1997-01-24

    Applicant: SAGAMI CHEM RES

    Inventor： KAMIMURA DAISUKE ,  YAMADA AKIHIRO ,  YAZAWA KAZUYOSHI

    IPC: C07C233/04 ,  A01N37/18 ,  C07C233/05 ,  C07C233/06 ,  C07C233/07 ,  C07C233/13

    Abstract: PROBLEM TO BE SOLVED: To obtain a new compound, having in vitro growth inhibiting activities against bacteria, capable of manifesting antifouling activities in the field, having especially high antimicrobial activities against marine attached bacteria and useful as an antimicrobial and antifouling agent. SOLUTION: This new compound is represented by the formula (R and R are each H, an aralkyl, etc.; X is Br or H), e.g. N-2-[(4-nitrophenyl) ethyl]tribromoacetamide. In the case of the N-2-[(4-nitrophenyl) ethyl]tribromoacetamide as an example, the compound represented by the formula is synthesized by adding thionyl chloride and N,N-dimethylformamide to tribromoacetic acid, carrying out the refluxing for 5hr, concentrating the reactional mixture, adding a mixture solution prepared by adding triethylamine to a solution of a 2-(4-nitrophenyl)ethylamine hydrochloride converted into a free amine in dichloromethane thereto under cooling with ice, conducting reaction at ambient temperature for 17hr, then adding a 20% aqueous solution of Na2 CO3 thereto, stirring the mixture, subsequently extracting the mixture with ethyl acetate, concentrating and purifying the resultant extract.

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