| 可逆性胆碱酯酶抑制剂——N,N-二甲胺基甲酸5-(1,2-取代苯骈咪唑)酯的合成 |
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| 引用本文： | 孟八一,纪庆娥.可逆性胆碱酯酶抑制剂——N,N-二甲胺基甲酸5-(1,2-取代苯骈咪唑)酯的合成[J].药学学报,1983,18(12):905-911. |
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| 作者姓名： | 孟八一 纪庆娥 |
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| 作者单位： | 军事医学科学院药理毒理研究所,北京 |
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| 摘 要： | 本文报道了用还原环合法制备1,2-二取代苯骈咪唑,并应用相转移催化反应于N-(4-甲氧基2-硝基苯基酰胺的N-烷化及5-羟基苯骈咪唑的二甲胺基甲酰化,合成了一系列N,N-二甲胺基甲酸5-(1,2-取代苯骈咪唑)酯,其碘甲烷季铵盐有一定的体外抑酶作用。
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| 关 键 词： | 1 2-取代苯骈咪唑 相转移催化 胆碱酯酶抑制剂 |
| 收稿时间： | 1982-07-19 |
SYNTHESIS OF AN TICHOLINESTERASES 5-(1, 2-SUBSTITUTED BENZIMIDAZOLYL)-N, N-DIMETHYI CARBAMATES |
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| MENG Ba-yi and JI Qing-e.SYNTHESIS OF AN TICHOLINESTERASES 5-(1, 2-SUBSTITUTED BENZIMIDAZOLYL)-N, N-DIMETHYI CARBAMATES[J].Acta Pharmaceutica Sinica,1983,18(12):905-911. |
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| Authors: | MENG Ba-yi and JI Qing-e |
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| Abstract: | A series of 5-(1,2-substituted benzimidazolyl)-N, N-dimethyl carbamates had been synthesized. The N-alkyl-4-methoxy-2-nitroanilides were converted into the 1,2-dialkyl-5-methoxy benzimidazoles by reductive cyclization. The technique of phase transfer cataiysis was successfully used in the N-alkylation of anilides and the N,N-dimethyl carbamylation of 5-hydroxybenzimidazoles.The bioactivity on cholinesterases of all these compounds have been tested. The methoiodides were found to be more active than the hudrochlorides. |
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| Keywords: | Phase transfer catalysis Anticholinesterase 1 2-Substituted benzimidazole |
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