Biologically active new 8.beta.-hydrazinomethyl-ergoline...

C - Chemistry – Metallurgy – 07 – D

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260/206.7

C07D 457/12 (2006.01) C07D 457/02 (2006.01)

Patent

CA 1120470

ABSTRACT OF THE DISCLOSURE The invention relates to new 8.beta.-hydrazinomethy-ergol- ine derivatives of the general formula (I), CH2-NH-NH-R1 Image (I) wherein x?y stands for a -CH2-CH- or -CH=C- group, R stands for hydrogen or methyl group, and R1 stands for hydrogen, a lower acyl group, a di-(lower)- alkylaminocarbonyl group, a group of the general formula (VI), Image (VI) wherein Z1, Z2 and Z3 each represent hydrogen, halogen or a trifluromethyl group, or a group of the general formula (VII), Image (VII) wherein Y represents a lower alkyl group, allyl group or phenyl group, and acids addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensiva - 2 - effects, furthermore they can be applied as starting sub- stances in the preparation of other biologically active ergoline derivatives. The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl- or -tosyloxymethly- ergoline derivatives with dry hydrazine. In order to obtain the N-substituted hydrazinomethyl compounds, the N-un- substituted derivatives are reacted with an acylating agent or with an isothiocyanate.

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