L Wang, LH Yun , QK Zhang, . SYNTHESIS OF OPTICAL ISOMERS OF2α-(2',2'- DISUBSTITUTED-2 'HYDROXYETHOXY)TROPANE AS POTENTIAL M-RECEPTOR ANTAGONISTSJ. Acta Pharmaceutica Sinica, 1996, 31(10): 790-794.
Citation: L Wang, LH Yun , QK Zhang, . SYNTHESIS OF OPTICAL ISOMERS OF2α-(2',2'- DISUBSTITUTED-2 'HYDROXYETHOXY)TROPANE AS POTENTIAL M-RECEPTOR ANTAGONISTSJ. Acta Pharmaceutica Sinica, 1996, 31(10): 790-794.
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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.
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