Abstract:
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 Ⅴ
1 and Ⅴ
4 could be catalytically hydrogenated smoothly to compounds Ⅵ
1 and Ⅵ
4, but compounds Ⅴ
2 and Ⅴ
3 could not in the same condition. And with 10% Pd/C in glacial acetic acid, Ⅴ
2 and Ⅴ
3 could be hydrogenated to Ⅵ
2 and Ⅵ
3. 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.