Synthesis of spiro [isobenzofuran-1 (3H), 4'-piperidines] as potential central nervous system agents. 1

VJ Bauer, BJ Duffy, D Hoffman, SS Klioze…

文献索引：Bauer; Duffy; Hoffman; Klioze; Kosley Jr.; McFadden; Martin; Ong Journal of Medicinal Chemistry, 1976 , vol. 19, # 11 p. 1315 - 1324

全文：HTML全文

被引用次数: 26

摘要

(MK-940). Convenient laboratory synthesis of 7a was provided by lithiation of 2- bromobenzhydryl methyl ether, followed by addition of 1-methyl-4-piperidone and acid- catalyzed cyclization. N-Dealkylation by standard methods afforded 9a. Synthesis of analogues was stimulated by discovery of marked inhibition of tetrabenazine-induced ptosis for lead compounds 7a and 9a. Optimal antitetrabenazine activity is associated with the S- ...