ビロリジン系薬理作用物質の合成研究(第10報)抗アセチルコリン作用物質1,1-Diethyl-および1,1-(epimeric)-Ethylmethyl-2-methyl-4-diphenylmethylenepyrrolidinium Iodidesの合成

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In the course of studies on the synthesis of pyrrolidine derivatives, which are analogous to Prifinium Bromide (1,1-diethyl-2-methyl-3-diphenylmethylenepyrrolidinium bromide (1) ; Padrin^[○!R], Riabal^[○!R]), we prepared the ethiodide (5) of 1,2-dimethyl-4-diphenylmethylenepyrrolidine, the methiodide (6) and the ethiodide (7) of 1-ethyl-2-methyl-4-diphenylmethylenepyrrolidine. We also present stereochemical data on diastereoisomeric quaternary pyrrolidinium salts 5 and 6,using nuclear magnetic resonance (NMR) spectroscopy. The anticholinergic action of 5,6 and 7 was 0.13,0.05,and 0.14,respectively in contrast to atropine which was defined as 1.00. There was no marked difference in the intensity of the action of the epimeric 1,1-ethylmethyl compounds 5 and 6.
公益社団法人日本薬学会の論文
1980-07-25