| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound useful in treatment of postmenopausal syndrome such as osteoporosis and estrogen-dependent breast cancer, fibroid uterus disease and endometritis and useful as an inhibitor for aortal smooth muscle cell proliferation. SOLUTION: This compound is represented by formula I [R<1> is H, OH, etc.; R<2> is H, a halo, etc.; R<3> is 1-piperidinyl, 4-morpholino, etc.; (n) is 2 or 3] or its salt, e.g. 1-[4-[29(1-piperidinyl)ethoxy]phenoxy-2-(4-hydroxyphenyl)-6- hydroxynaphthalene hydrochloride. The compound is obtained by aromatizing a ketone of formula II [R<1a> is H or OR<5> (R<5> is a hydroxy-protecting group; R<2a> is a halo or OR<6> (R<6> is R<5> ), etc.], to convert the ketone to phenol, reacting the phenol derivative with a 4-halobenzaldehyde to afford a new biaryl ether and then, treating a new intermediate of formula III obtained from the compound with a compound of the formula R<3> -(CH2 )n -Q (Q is Br or Cl). |
