Process for the preparation of pyridoindole derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01)

Patent

CA 1146942

ABSTRACT "PROCESS FOR THE PREPARATION OF PYRIDOINDOLE DERIVATIVES" Pyridoindole derivatives of formula Image (I) n = 0 or 1; R1 = H, Hal, alk, alk-O-, CF3; R2 = -COOalk, -CONHR5 (R5 = H or various substituents); R3 = H, alk, -COOalk; R4 = H, Ac, alk, -CONHR6 (R6 = H or various substituents), and acid addition salts, except certain known compounds, are useful in treating anoxia and depression and in psychotropic therapy. They are prepared from tryptamine or a derivative thereof by reaction thereof with a pyruvic ester or 3-ethoxycarbonyl- 1,2-dioxo-1-ethoxypropane to form compounds in which R4 is H and R2 is -COOalk. These compounds are reacted with amines, isocyanates or usual N-acylating or N-alkylating reagents to prepare the other compounds.

343697

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