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
-
Abstract: 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.
下载: