鎮痙作用を有する芳香族塩基性エーテルに関する研究(第1報)3-(N, N-Disubstituted Amino)-1-phenylpropyl Phenyl Ether誘導体の合成と抗Ach作用

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Several kinds of 3-(N, N-disubstituted amino)-1-phenylpropyl phenyl ethers were prepared according to the reaction scheme shown in Chart 1 (Substituted amino groups were dimethylamino, diethylamino, diisopropylamino, piperidino, morpholino, methylpiperidino, etc.). A related compound having a sulfonium group instead of amino group was also synthesized. In the case of 3-(2-methylpiperidino)-1-phenylpropyl phenyl ether and 3-(2-ethylpiperidino)-1-phenylpropyl phenyl ether, two kinds of diastereoisomers were respectively separated. The anticholinergic and mydriatic activities of 28 new compounds were examined. Piperidino, 2-ethylpiperidino, and 2-methylpiperidinopropyl phenyl ether derivatives showed a stronger activity than other compounds.
1973-04-25