4-(1-isoquinolyl)-piperidin-4-ol compounds and their...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) A61K 31/47 (2006.01) C07D 211/04 (2006.01) C07D 217/04 (2006.01) C07D 211/06 (2006.01)

Patent

CA 1073910

ABSTRACT OF THE DISCLOSURE Isoquinolines of the formula Image wherein R1 is H or alkyl of 1 - 4 carbon atoms, R2 is H and R3 is OH, or R2 and R3 collectively are a C-C bond, and physio- logically acceptable acid addition salts thereof have anti depressant activity. These isoquinolines can be prepared by solvolyzing or hydrogenolyzing a compound of the formula Image or an acid addition salt thereof, wherein R4 is R1 or R6, R5 is OR7 or, when R4 is R6, is R3; R6 and R7 are radicals which can be split off solvolytically or hydrogenolytically and R1 and R2 are as above. A resulting carbinol (R2 is H, R3 is OH) may be dehydrated; and/or a resulting compound (R1 is H) may be treated with a N-alkylating agent; and/or a resulting base may be converted to a physiologically acceptable acid addition salt by treatment with an acid.

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