GB1219606A — Quinuclidinol derivatives and preparation thereof

USPTO Abstract

1,219,606. Esters of 3-quinuclidinol. SOC. GENERALE DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (SOGERAS). 14 July, 1969 [15 July, 1968], No. 33654/68. Heading C2C. The invention comprises compounds of formula wherein R is H, OH or C 1-4 alkyl, R 1 is Ph or thienyl, and R 2 is cyclohexyl, cyclopentyl or thienyl, or when R is H, R 1 R 2 C froms a 9-(9,10) dihydroanthryl, 9-xanthyl or 9-thioxanthyl group; and acid addition and quaternary ammonium salts thereof. These compounds may be prepared by transesterification of the corresponding methyl or ethyl esters (R= OH) with 3- quinuclidinol; or by reacting the corresponding acid chlorides (R#OH) with 3-quinuclidinol (or e.g. its Na salt). Therapeutic compositions for oral, parenteral or rectal administration, comprise compounds of the above formula, which are stated to be useful where atropine antispasmodics and central anticholinergic agents are indicated.