biologically active derivatives of 8 beta idrazinometil - ergolina and process for their preparation

摘要

The invention relates to new 8 beta -hydrazinomethyl-ergoline derivatives of the general formula (I), IMAGE (I) wherein x y stands for a IMAGE or IMAGE 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 trifluoromethyl group, or a group of the general formula (VII), IMAGE (VII) wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances 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 -tosyloxymethyl-ergoline derivatives with dry hydrazine. In order to obtain the N-substituted hydrazinomethyl compounds, the N-unsubstituted derivatives are reacted with an acylating agent or with an isothiocyanate.