Biologically active new 8.beta.-hydrazinomethyl-ergoline derivatives and a process for the preparation thereof
US4235912A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 19, 1979 |
| Grant date | Nov 25, 1980 |
| Priority date | — |
| Expiry date | Mar 19, 1999 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P43/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, and PA0 R.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.