| 摘要 |
<p>1423065 D-6-Methyl-2,8-disubstituted ergoline ELI LILLY & CO 10 July 1973 [21 July 1972] 32890/73 Heading C2C Novel D-6-methyl-2,8-disubstituted ergoline compounds of the Formula (I) wherein X is halo, methyl or CN and R is CH 2 CN or CH 2 CONH 2 and their salts formed with pharmaceutically acceptable acids may be obtained (where X is halo) by reacting a compound of formula wherein R<SP>1</SP> is Cl, Br, I, O-SO 2 -CH 3 or O-SO 2 -p-tolyl; with a positive halogenating agent containing positive chlorine, bromine or iodine, to yield a compound of formula and then reacting this with an inorganic cyanide in an inert solvent. Conversion of the cyano group to the amide can be effected by well known procedures. Compounds in which X is CH 3 can be prepared by reacting D-6-methyl- 8-cyanomethyl (or 8-carboxamidomethyl)ergoline with methyl formate and ethanedithiol to form a dithioethylene acetal and desulphurizing the latter to form the 2-methyl derivative. Compounds in which X is CN can be prepared by reaction of a 2-unsubstituted ergoline with chlorosulphonylisocyanate and triethylamine. Pharmaceutical composition for inhibiting the secretion of prolactin in mammals contains as active ingredient a compound of Formula (I) or a salt thereof in forms suitable for oral or parenteral administration.</p> |
