4-Amino-4-arylcyclohexanones and their derivatives, a novel class of analgesics. 1. Modification of the aryl ring

…, PF Von Voigtlander, DE Emmert

文献索引：Lednicer, Daniel; VonVoigtlander, Philip F.; Emmert, D. Edward Journal of Medicinal Chemistry, 1980 , vol. 23, # 4 p. 424 - 430

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被引用次数: 32

摘要

Investigation of central nervous system activity of phenylcyclohexylamines was continued by preparation of" reversed" analogues. Following the unexpected finding of analgesic activity with 1-(dimethylamino)-1-phenylcyclohexylamine, the SAR of the series was investigated. Synthesis starts by double Michael reaction of acrylate on arylacetonitriles. Following cyclization, decarboxylation, ketalization, and saponification, the geminally substituted ...