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新型地氯雷他定酰胺衍生物的合成及其利尿活性

Xiao-shuai XIE,Shuai MU,Chu-bing TAN,Zhi-xing ZHOU,Deng-ke LIU,Wei-ren XU

Chinese Journal of Synthetic Chemistry（2014）

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Abstract
以地氯雷他定和对硝基苯甲酰氯为原料,三乙胺为缚酸剂,经N-酰化反应制得{4-[8-氯-5H-苯并[5,6]环庚并[1,2-b]吡啶-11(6H)-亚基]哌啶-1-基}(4-硝基苯基)甲酮(3);3在酸性条件下经SnCl2还原得中间体(4).以吡啶为缚酸剂和溶剂,4与烷基酰氯(或苯酰氯)经酰化反应合成了7个具有潜在AVP-V2受体拮抗活性的新型地氯雷他定酰胺衍生物(6a～6g),其结构经1H NMR和HR-MS表征.SD大鼠利尿活性实验表明,6a～6g均有一定的利尿活性,其中N-[4-{4-[8-氯-5H-苯并[5,6]环庚烷并[1,2-b]吡啶-11(6H)-亚基]哌啶-1-羰基}苯基]丙酰胺的利尿活性与托伐普坦相当.
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Desloratadine,amide derivative,AVP-V2 receptor antagonist,synthesis,diuretic activity
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