胆碱能M受体拮抗剂：2α－（2＇，2＇－二取代基－2＇－羟基乙氧基）托品烷光学异构体合成  

SYNTHESIS OF OPTICAL ISOMERS OF2α-(2',2'- DISUBSTITUTED-2 'HYDROXYETHOXY)TROPANE 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：《药学学报》1996年第10期790-794,共5页Acta Pharmaceutica Sinica

摘　　要：胆碱能Ｍ受体拮抗剂：２α－（２＇，２＇－二取代基－２＇－羟基乙氧基）托品烷光学异构体合成王林，恽榴红，张其楷（军事医学科学院毒物药物研究所，北京１００８５０）目前临床所用托品类抗胆碱药一般为３位取代托品酯类衍生物，这类药物作用较广泛，但选择性不高。Ａ...Eight 2α-(2',2'-disubstituted-2'-hydroxyethoxy) tropanes(2)were prepared byreactions of enantiomeric and racemic 2α-tropanols with 1,1-disubstituted oxiranes.The optical purityof these diastereoisomers was analyzed by RP-HPLC. The results of preliminary screening indicatedthat the stereochemical variations of these isomers exhibited great influence on the binding affinity forrat brain M-receptor Compounds with 2' R configuration for the tertiary carbon showed greateractivity.

关 键 词：M受体拮抗剂 胆碱能 托品醚 光学异构体 

分 类 号：TQ463[化学工程—制药化工] R971.92[医药卫生—药品]