GB865974A - Manufacture of new phenyl-quinuclidines - Google Patents

Abstract

The invention comprises 3-phenyl-quinuclidine compounds containing either a saturated or D 2-unsaturated quinuclidine nucleus free from further substituents, and whose phenyl residue is unsubstituted or substituted by a dialkylamino group, their acid addition and quaternary ammonium salts; and the preparation thereof by treating a 3-phenyl-3-hydroxy-quinuclidine with a dehydrating agent, and, if desired, hydrogenating the D 2-quinuclidine so obtained, and, if desired, converting a base so obtained into an acid addition or quaternary ammonium salt, or converting a salt so obtained into the free base. The products are useful as central nervous system stimulants (see Group VI).ALSO:Pharmaceutical preparations useful as central nervous system stimulants contain a 3-phenyl-quinuclidine compound having either a saturated or D 2-unsaturated quinuclidine nucleus free from further substituents, and whose phenyl residue is unsubstituted or substituted by a dialkylamino group, or an acid addition or quaternary ammonium salt thereof, in admixture with a pharmaceutical organic or inorganic carrier suitable for enteral, parenteral or topical administration. They may be in the form of creams, dragees, emulsions, salves, solutions, suspensions or tablets; and, if desired, they may be sterilized and/or contain auxiliary substances such as emulsifying, preserving, stabilizing or wetting agents, salts for regulating asmotic pressure or buffers. Other therapeutically active substances may be incorporated. Specified salts are hydrohalides, sulphates, nitrates, phosphates, thiocyanates, perchlorates, acetates, propionates, oxalates, malonates, succinates, malates, methane-, ethane-, hydroxyethane-, benzene- and toluene-sulphonates, picrates, salts with therapeutically active acids, and quaternary ammonium salts formed by the action of alkyl halides or sulphonates or dialkyl sulphates.