Process for the preparation of ergoline derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 457/00 (2006.01) C07D 457/02 (2006.01) C07D 457/06 (2006.01)

Patent

CA 1191840

ABSTRACT OF THE DISCLOSURE Process for preparing ergoline derivatives of formula: Image I wherein n=0, 1, 2; R1=H, CH3; R2=H, CH3, halogen; R3=H, OCH3; R4=hydrocarbon group and R5 is a residue of general formula II, III, IV, V, VI, VII: Image Image Image II III IV Image Image Image V VI VII wherein R6=H, Cl, OCH3, NR11R12, wherein R11 and R12=H, lower alkyl; phenyl or are bonded together to form a heterocyclic, ring, R7, R8 and R9 and R10=H or C1-C3 alkyl, with the proviso that if R5 is of formula II and R2=R7=R8=H, then R4 is not methyl or n is not 0, and pharmaceutically acceptable acid addition salts thereof, charac- terized by reaction of mixed anhydride of the appropriate 8-carboxy ergoline with an amine. The compounds have anti- depressive, anti-hypertensive and antiprolactin activity.

407645

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