Synthesis and analgesic activity of pyrrolidinomorphinan derivatives

被引：0

作者：

Shul'ts E.E. ^{[1
]}

Tolstikova T.G. ^{[1
]}

Tolstikov S.E. ^{[1
]}

Daibova V.T. ^{[1
]}

Shakirov M.M. ^{[1
]}

Bolkunov A.V. ^{[1
]}

Dolgikh M.P. ^{[1
]}

机构：

[1] Vorozhtsov Institute of Organic Chemistry, Siberian Division, Russian Academy of Sciences, Novosibirsk

来源：

Pharmaceutical Chemistry Journal | 2007年 / 41卷 / 2期

基金：

俄罗斯基础研究基金会;

关键词：

Analgesic Activity; Thebaine; Morphinan; Ammonium Hydroxide Solution; Aryl Moiety;

D O I：

10.1007/s11094-007-0016-3

中图分类号：

学科分类号：

摘要：

Diels-Alder reactions of (-)-thebaine with N-substituted maleimides have been used to obtain cycloadducts possessing α-facial stereoselectivity. The 3-O-and 6-O-demethylated derivatives as well as the products of complete and partial reduction of carbonyl groups in the pyrrolidinedione moiety were also obtained. Some of the synthesized compounds have proved to be promising analgesics. The introduction of the bromine atom into the aryl moiety favors prolongation of the analgesic effect. © 2007 Springer Science+Business Media, Inc.

引用

页码：74 / 77

页数：3

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