| 摘要 |
The pyrroloisoquinolines of the formula <CHEM> wherein R1 and R2, independently, are hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl or alkenyl, or taken together are alkylene of 3 to 6 carbon atoms; and R3 is hydrogen, alkyl, hydroxyalkyl, phenylhydroxyalkyl, halophenylhydroxyalkyl, alkylphenylhydroxyalkyl, alkoxyphenylhydroxyalkyl, alkoxyalkyl, aryloxyhydroxyalkyl, alkoryhydroxyalkyl, acyloxyalkl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkylcycloalkyl, alkynyl, thienylalkyl, furylalkyl, arylcarboxamidoalkyl, acylalkyl, cycloalkyloxyalkyl, cycloalkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, or aryl-N-imidazolonylalkyl; R4 is alkyl; and n is the integer 2 or 3, their corresponding optical isomers, geometric isomers, and mixtures thereof, and their pharmaceutically acceptable acid additional salts, are long-acting prodrugs of known antipsychotic agents which are obtained by enzymatic cleavage of the N-pyrrolo acyl moiety. The compounds of formula I themselves exhibit antipsychotic activity end can be prepared by acylating the pyrrolo nitrogen atom. |
