哌替啶非对映异构体2-甲基反式酯的酚类类似物。

Phenolic analogues of diastereoisomeric 2-methyl reversed esters of pethidine.

作者信息

Casy A F, Dewar G H, Pascoe R A

机构信息

School of Pharmacy and Pharmacology, University of Bath, UK.

出版信息

J Pharm Pharmacol. 1989 Mar;41(3):209-11. doi: 10.1111/j.2042-7158.1989.tb06434.x.

DOI:10.1111/j.2042-7158.1989.tb06434.x

PMID:2568454

Abstract

The preparation and stereochemical characterization of alpha- and beta-isomers of 1,2-dimethyl-4-m-hydroxyphenyl-4-propionyloxypiperidine are described. Both the alpha (axial 4-aryl/chair) and beta (equatorial 4-aryl/chair) isomers were of low potency or inactive in mice antinociceptive tests. Shortcomings of the alpha-isomer as a model for the 4-arylpiperidine moiety of morphine are discussed.

摘要

描述了1,2 - 二甲基 - 4 - 间羟基苯基 - 4 - 丙酰氧基哌啶的α - 和β - 异构体的制备及立体化学特征。α - 异构体（4 - 芳基轴向/椅式）和β - 异构体（4 - 芳基赤道向/椅式）在小鼠抗伤害感受试验中均效力低或无活性。讨论了α - 异构体作为吗啡4 - 芳基哌啶部分模型的不足之处。