Synthesis and Pharmacological Activity of gem-Dialkyl-9-azabicyclo [3,3,1] nonane Derivatives : New Anti-Cholinergic Agent

概要

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6,6-and 7,7-dialkyl-9-alkyl-9-azabicyclo [3,3,1] nonan-3-one (V) and (IX), synthesized from 2,2-and 3,3-dialkylglutaraldehyde by the Robinson-Schopf reaction, were reduced with NaBH_4 and Na-EtOH to afford the A-and B-isomers of the corresponding 6,6-and 7,7-dialkyl-9-alkyl-9-azabicyclo [3,3,1] nonan-3-ol (VI) and (X), respectively. Hydroxy groups on 3-position of A-and B-isomer of the alcohols were confirmed to be α-and β-configuration by the formation of a tetrahydrooxazine ring, respectively. Various ester and carbamate compounds of the alcohols (VI) and (X) were synthesized and their pharmacological activities were studied. Among their compounds several glycolate derivatives had a potent anti-cholinergic activity and showed high central specificity.
社団法人日本薬学会の論文
1972-03-25