Merz & Co.

Dezso Peteri

Arthur Scherm

Certain 1,3,5-trisubstituted adamantane compounds having central nervous system activity, especially anti-Parkinsonism activity, method of preparing same, and pharmaceutical compositions thereof, method of influencing the central nervous system therewith.

Drugs or medicines for influencing the central nervous system

The application discloses a novel improved process for the production of .alpha.-[2-(p-chlorophenoxy)-isobutyl]-.beta.-nicotinoyl glycol ester, a known compound having a lipid-lowering effect, by the reaction of .alpha.-[2-chlorophenoxy)-isobutyryl]-.beta.-ethyl chloride ester with an alkali salt of nicotinic acid, preferably sodium nicotinate, preferably in a high-boiling polar or dipolar aprotic solvent, especially dimethylformamide, most preferably at a temperature of about 120.degree. - 180.degree. C., and most advantageously in refluxing dimethylformamide. An unpredictable increase in yields of the desired product over yields attainable by previously-available processes is thereby obtained.

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Munich, Georgia

Dezso Peteri