| 摘要 |
This invention is related to the following compounds: ¢3 (3-bromopropoxy)-4-methoxyphenyl! phenylmethanone, 6-chloro-3- (1-piperazinyl)-1H-inadazole, 1-¢4-(3-bromopropoxy)-3-bromophenyl! ethanone, 1-¢4-(3-bromopropropoxy)-3,5-dibromophenyl!ethanone, 1-¢4-(3-bromopropoxy)-3- (methylmercapto)phenyl! ethanone, 4-(3-bromopropoxy)-3-methoxybenzonitrile, 1-¢4-(3-bromopropoxy)-3-methylphenyl!ethanone, 1-¢4-(3-bromopropoxy)-3-methoxyphenyl! phenylmethanone. The aforementioned compounds are useful as synthetic intermediates in the synthesis of pharmaceutically active compounds of the formula: <IMG> wherein X is -O-, -S-, <IMG>, or <IMG>; p is 1 or 2; Y is hydrogen, C1 to C6 alkyl, -OH, Cl, F, Br, I, C1 to C6 alkoxy, -CF3, -NO2, or -NH2, when p is 1; Y is C1 to C6 alkoxy when p is 2 and X is -O-; R2 is selected from the group consisting of lower alkyl, aryl lower alkyl, aryl, cycloalkyl, aroyl, alkanoyl, and phenyl sulfonyl groups; Z is -CH- or -N-; n is 2, 3, 4, or 5; R is hydrogen, alkyl, C1 - C6-alkoxy, hydroxyl, carboxyl, Cl, F, Br, I, amino, C1 - C6-mono or-dialkyl amino, -NO2, lower alkyl thio, -OCF3, cyano, acylamino, -CF3, trifluoroacetyl, aminocarbonyl, <IMG> alkyl is lower alkyl: aryl is phenyl or <IMG> R1 is hydrogen, lower alkyl, C1 - C6 alkoxy, hydroxy, Cl, F, Br, I, C1 - C6 alkyl amino, -NO2, -CN, -CF3, -OCF3; and heteroaryl is where <IMG>; Q is -O-, -S-, <IMG>, -CH=N; R3 is hydrogen, lower alkyl, or acyl; and m is 1, 2, or 3; or a pharmaceutically acceptable acid addition salt thereof. The invention relates further to a process for the preparation of the above compounds and their use as medicaments having antipsychotic and/or analgetic activity.
|
