胆碱能M受体拮抗剂2β－（2－环戊基－2－羟基－2－苯基乙氧基）托品烷光学异构体的合成  

Synthesis of Enantiomeric 2β-(2-Cyclopentul-2-Hydroxy-2-Phenylethoxy) Tropanes as Potential M Receptor Antagonists

作　　者：王林[1] 恽榴红[1] 张其楷[1] 

机构地区：[1]军事医学科学院毒物药物研究所

出　　处：《中国药物化学杂志》1996年第2期94-99,共6页Chinese Journal of Medicinal Chemistry

摘　　要：以（１Ｓ）－（＋）－１０－樟脑磺酸－２Ｒ－和－２Ｓ－２－环戊基－２－羟基－２－苯基乙醇酯分别与１Ｒ，２Ｓ和１Ｓ，２Ｒ－托品醇反应，制备了四个不同构型的２β托品醚目标化合物．大鼠脑Ｍ受体结合试验表明，异构体之间活性差异显著，最大相差约２２０倍。当分子中季碳为Ｒ构型时，对活性影响最大。Four diastereoisomers of 2β-(2-cyclopentyl-2-hydroxy-2-phenylethoxy) tropanes(1) were prepared respectively by reactions of enantiomeric 1R, 2S and 1S, 2R-tropanols with 2R and 2S-(2-cyclopentyl-2-hydroxy-2-phenyl) ethyl-(1S)-(+)-10-camphorsulfonates. The results of preliminare pharmacology indicated that the stereochemical variations of these isomers had great influence on the binding affinity for the rat brain M receptor. Compound(1b) and (1c) with 2R configuration in tertiary carbon had greater activity.

关 键 词：胆碱能M受体 拮抗剂 2β-托品醚 光学异构体 

分 类 号：TQ463.4[化学工程—制药化工]