ANTICHOLINERGICS:SYNTHESIS OF 2',2'-DIPHENYLETHYL AZACYCLOALKANE DERIVATIVES

3-Quinuclidinyl, N-methylpiperidin-4-yl, N-benzylpiperidin-4-yl, N-methyl-3-azabicyclo (3,3,1)nonan-9-yl, which were found in molecular structures of some stronger anticholinergics, were selected to displace tropanyl in 3-(2′, 2′-diphenylethyl) tropane (L) and its derivatives Twelve compounds (Ⅳ_1～4,Ⅴ_1～4, Ⅵ_1～4) were synthesized. With Raney Ni in ethanol, compounds Ⅴ₁ and Ⅴ₄ could be catalytically hydrogenated smoothly to compounds Ⅵ₁ and Ⅵ₄, but compounds Ⅴ₂ and Ⅴ₃ could not in the same condition. And with 10% Pd/C in glacial acetic acid, Ⅴ₂ and Ⅴ₃ could be hydrogenated to Ⅵ₂ and Ⅵ₃. Animal tests (mydriasis, antisalivary secretion and antiarecoline tremor) showed that the anticholinergic activities of these compounds were weaker than those of the lead compound (L) and atropine.