2h-azeto¬2,1-a|-isoquinoline derivatives, process for their...

C - Chemistry – Metallurgy – 07 – D

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167/241, 260/271

C07D 455/00 (2006.01) A61K 31/395 (2006.01) C07D 463/00 (2006.01)

Patent

CA 1253156

ABSTRACT OF THE DISCLOSURE New 2H-azeto[2 ,1-a]-isoquinoline derivatives of the formula: Image (I) are disclosed wherein R1 and R2 each represents hydroxyl or alkoxy having from 1 to 6 carbon atoms, R3 is hydroxyl, halogen or an -O-?-R4 group, wherein X is oxygen or sulfur, and R4 is phenyl, and acid addition, metal and quaternary salts thereof. The new compounds are prepared by cyclization of the corresponding compounds of formula: Image (II) wherein R1, R2 and R3 are as defined above, and Hal is halogen. Compounds of formula (I) are pharmaceutically active, in particular are potent analgesic and antipyretic agents.

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