【摘要】 芬太尼类化合物有很高的镇痛活性，4-甲氧羰基芬太尼是其中镇痛活性最强的化合物，其镇痛活性为吗啡的10031倍，过去的几十年，该类化合物的合成、镇痛活性及构效关系的研究引起了极大的关注，本文综述了4-甲氧羰基芬太尼类化合物的研究进展。

    【关键词】 药物化学；构效关系；综述；4-甲氧羰基芬太尼；合成方法；镇痛活性

    Synthesis and structure-activity reactionship of 4-methoxycarbonyl fentanyl derivatives

    YANG Chun-xia，HU Wen-xiang.

    Department of Chemistry，the Institute of Physical Organic and Medicinal Chemistry，Capital Normal University，Beijing 100037，China

    【Abstract】 The fentanyl derivatives have powerful analgesic activity.The greatest compound is 4-methoxycarbonyl fentanyl and its analgesic activity is 10031 multiples(morphine=1).In the past several decades，people have great interest in synthesis，analgesic activity and structure-activity relationship of 4-methoxycarbonyl fentanyl derivatives.In this paper，the research progress of 4-methoxycarbonyl fentanyl derivatives was summarized.

    【Key words】 medicinal chemistry; SRA; review; 4-methoxycarbonyl fentanyl; synthesis; analgesic activity

    20世纪60年代初Janssen等首次报道了新型强效镇痛药芬太尼[1]，此后对该类镇痛药的研究及应用受到了极大的重视。2002年俄罗斯在莫斯科轴承厂文化宫解救人质时，就使用了芬太尼类强效镇痛性失能剂。芬太尼是著名的高效麻醉性镇痛药 ......