GB865973A - Manufacture of phenyl-quinuclidines - Google Patents

Abstract

The invention comprises 3-phenyl-3-hydroxyquinuclidines of the general formula: <FORM:0865973/IV (b)/1> (wherein Ph represents a phenyl or dialkylaminophenyl group) and their acid addition salts and quaternary ammonium compounds, and the preparation thereof by reacting a 3-quinuclidone with a correspondingly substituted or unsubstituted phenyl-metal compound, and, if desired, converting a base so obtained into an acid addition salt or a quaternary ammonium compound 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-3-hydroxyquinuclidine of the general formula <FORM:0865973/VI/1> (wherein Ph represents a phenyl or dialkylaminoalkyl 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 osmotic pressure or buffers. Other therapeutically active substances may be incorporated. Specified salts are hydrohalides, sulphates, nitrates, phosphates, thiocyanates, 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.