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.