摘要:
Ergoline derivatives are disclosed having the general formula ##SPC1##Wherein R is selected from the group consisting of a lower alkyl radical having from 1 to 4 carbon atoms; an --NH-lower alkyl radical having from 1 to 4 carbon atoms; a free or substituted phenyl- or 2-furanoyl radical; the --O--CH.sub.2 --C.sub.6 H.sub.5 radical; a (3)- or (4)-pyridine radical free or substituted by a methyl radical or a chlorine or bromine atom; a pyrrole radical of formula ##SPC2##WhereinY is hydrogen, a lower alkyl radical having from 1 to 4 carbon atoms or phenyl;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, methyl or halogen; andR.sub.3 and R.sub.4 are the same or different and are hydrogen, halogen, a lower alkyl radical having from 1 to 4 carbon atoms, carbethoxy, or a lower alkyloxy radical having from 1 to 4 carbon atoms.Novel processes for the preparation of these compounds are also disclosed.
摘要:
.alpha.-D-6-methylergolinyl-8-acetamides of the formula: ##SPC1##Are readily prepared from .alpha.-D-6-methylergolinyl-8-acetic acid azide hydrochloride and amines of the formula R.sub.1 -NH-R.sub.2 and may be converted to their salts with inorganic and organic acids by neutralization. In these formulas, R.sub.1 may be hydrogen or lower alkyl, R.sub.2 may be hydrogen, lower alkyl, cycloalkyl having 5 or 6 carbon atoms, hydroxyalkyl having 3 or 4 carbon atoms, or lower alkoxycarbonylmethyl or R.sub.1 and R.sub.2 jointly may be divalent alkylene having 4 or 5 C atoms. The salts of most of these bases with physiologically tolerated acids are nontoxic in doses which suppress lactatical and prevent pregnancy in rats when applied orally after copulation. The others, equally non-toxic, extend the effective period of thiopental.
摘要:
6-methyl-8-alkoxymethylergolines are prepared by reaction of a 6-methyl-8-(substituted)methylergoline with a benzyl quaternary ammonium alkoxide. 6-Methyl-8-phenoxymethylergolines are prepared by reaction of an 8-(substituted)-methylergoline with phenol in the presence of strong base. The new 8-oxymethylergolines of this invention are useful as prolactin inhibitors.
摘要:
THIS INVENTION CONCERNS THE NEW COMPOUND, (5R,8R)8 - (3-AZABICYCLO(3,2,2)NONAN-3-YLMETHYL) - 6 - METHYLERGOLENE, USEFUL AS A SEDATIVE AND SLEEP-PROMOTING AGENT.
PREPARED BY REACTING D-6-METHYL-8-HYDROXYMETHYLERGOLINE (I) WITH PHOSPHORYL CHLORIDE AND THEREAFTER REACTING THE D-6-METHYL-8-CHLOROMETHYLERGOLINE FORMED WITH AN ALKALI METAL CYANIDE. THE COMPOUNDS OF THE INVENTION CONSTITUTE ANTIFERTILITY AND LACTATION INHIBITING AGENTS.