发明名称 NOVEL PRODUCTION METHOD OF BENZOIC ACID DERIVATIVE
摘要 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.
申请公布号 JP2000034262(A) 申请公布日期 2000.02.02
申请号 JP19990203717 申请日期 1999.07.16
申请人 SHUDO KOICHI 发明人 HAMADA YOSHINORI;YAMADA ISAMU;KAMINAKA MASAO;SAKATA TERUO
分类号 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 主分类号 A61K31/00
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