abstract |
PURPOSE: To obtain a new aryl deriv. which is useful for the treatment for inflammatory or allergic diseases induced by catalytic oxidation of arachidonic acid with 5-lipoxigenase, by coupling specified two kinds of compds. n CONSTITUTION: A compd. expressed by formula I is subjected to coupling reaction with a compd. expressed by formula II in the presence of a base in an inert solvent with addition of a catalyst, preferably at 100°C to obtain the objective compd. expressed by formula III. The compd. expressed by formula III is, for example, 4-[3-(4-(4-fluorobenzyl)phenylthio)phenyl]-4- methoxytetrahydropyran. In formula I, Ar 1 is phenyl, naphthyl, etc.; X 1 is oxy, thio, sulfinyl, etc.; Ar 2 is halogen, hydroxy, etc.; X 2 is oxy, thio, etc. In formula II, R 1 is 1-4C alkyl, 3-4C alkenyl, etc.; R 2 and R 3 may be bonded to form -A 1 -X 3 -A 2 (wherein A 1 , A 2 are 1-3C alkylene and form a 5 to 7-membered ring with the carbon atom bonded; X 3 is oxy, thio, etc. n COPYRIGHT: (C)1992,JPO |