Isoquinoline derivatives

Details Isoquinoline derivatives Isoquinoline derivatives

C - Chemistry, Metallurgy

07

D

260/246.1, 260/2

C07D 471/04 (2006.01) C07D 209/08 (2006.01) C07D 217/04 (2006.01)

Patent

CA 1132553

Abstract Octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula Image A wherein R1 is hydrogen, alkyl, alkanoyl, aroyl or aralkyl; R2 and R3, independently, are hydrogen, alkyl, cycloalkyl, alkenyl, acyl, aryl or aralkyl; and R4 is hydrogen, alkyl, hydroxyalkyl, phenyl-hydroxyalkyl, halophenyl-hydroxyalkyl, alkylphenyl-hydroxyalkyl, alkoxyphenyl-hydroxyalkyl, alkoxy- alkyl, aryloxy-hydroxyalkyl, alkoxy-hydroxyalkyl, acyloxyalkyl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkyl- cycloalkyl, alkynyl, thienyl-alkyl, furyl-alkyl, arylcarboxamido- alkyl, acylalkyl, cyclic-alkyloxoalkyl, cyclic-alkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, N-alkyl-pyrrolidinylalkyl, trifluoroalkyl of 2 to 6 carbon atoms, aryl-N-imidazolonylalkyl, or Image , wherein R6 and R7, independently, are hydrogen or alkyl, or taken together with the nitrogen, are a 5- or 6-membered heterocyclic ring, and X is O or S, optical and geometric isomers of these compounds and pharmaceutically aceptable acid addition salts thereof possess valuable neuroleptic/ antipsychotic activities, and thus, can be used for the treatment of schizophrenia. These compounds can be prepared according to different processes.

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