PURPOSE: To provide the new compound reduced in the adverse actions such as muscular relaxation actions and useful as a selective antianxiety agent.
CONSTITUTION: A compound of formula I [R1 is carboxyl, formyl, cyano, acyl, etc.; R2 is H, 1-8C alkyl, hydroxyalkyl, substituted aryl, aralkyl, etc.; A is S, -CH=CH-; E is -CH2-, -S(O)m- ((m) is 0-2); (n) is 1, 2; the bond represented by the full line and the dotted line is a single bond or double line; but when A is S, E is -CH2-, and when A is -CH=CH-, E is -S(O)m- and (n) is 2]. For example, 8-acetyl-2-(4-chlorophenyl)-4,4a,5,6-tetrahydrothieno[2,3-h]cinnoline-3(2H)-one. The compound of formula I is obtained e.g. by reacting a compound of formula II with a compound of formula III (R3 is alkyl, haloalkyl, etc.) in the presence of a dehydrating agent such as polyphosphoric acid.
TANAKA HIROSHI
MORIMOTO YASUTO
TAKEHARA SHUZO
