| 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 |
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| 引用本文： | 王林,恽榴红,张其楷. 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[J]. 药学学报, 1996, 31(10): 790-794 |
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| 作者姓名： | 王林 恽榴红 张其楷 |
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| 作者单位： | 军事医学科学院毒物药物研究所 |
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| 摘 要： | 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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| 关 键 词： | 2α-托品醚 光学异构体 M受体桔抗剂 反相高效液相色谱法 |
| 收稿时间： | 1995-09-05 |
SYNTHESIS OF OPTICAL ISOMERS OF2α-(2',2'- DISUBSTITUTED-2 'HYDROXYETHOXY)TROPANE AS POTENTIAL M-RECEPTOR ANTAGONISTS |
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| L Wang,LH Yun and QK Zhang. SYNTHESIS OF OPTICAL ISOMERS OF2α-(2',2'- DISUBSTITUTED-2 'HYDROXYETHOXY)TROPANE AS POTENTIAL M-RECEPTOR ANTAGONISTS[J]. Acta pharmaceutica Sinica, 1996, 31(10): 790-794 |
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| Authors: | L Wang LH Yun QK Zhang |
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| 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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| Keywords: | Optical isomers M-receptor antagonists RP-HPLC 2α- tropane ethers |
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