摘要/Abstract

吲哚衍生物因其可以亲和多种受体而被认为是设计药物先导化合物的优势结构.其中，3-吲哚羧酸酯类化合物是广泛存在于天然产物及药物分子中的重要的结构单元，如盐酸阿比多尔、托烷司琼、PD 0298029、Grandilodine A等均为3-吲哚羧酸酯类药物分子或天然产物.基于此，近年来关于3-吲哚羧酸酯类化合物及其衍生物的合成不断地被报道，金属催化的以及非金属条件下的合环反应用来构建吲哚中的吡咯环是近年来研究的热点，而在吲哚C-3位直接进行官能团化合成酯基官能团同样具有较高的效率.在相关研究的基础上，按照上述分类方法，综述了近年来3-吲哚羧酸酯类化合物的合成研究进展.
关键词: 3-吲哚羧酸酯, 金属催化合环, 碳氢官能团化, 无过渡金属反应, 合成进展
Indole derivatives have been considered as “privileged scaffolds” in drug discovery since they are capable of binding many receptors with high affinity. 3-Indolecarboxylates are widespread structure motifs in many natural products and drug molecules, such as arbidol, tropisetron, PD 0298029, and grandilodine A, etc. Consequently, synthetic studies toward 3-indolecarboxylates have been reported in recent years. Elegant cyclization strategies have been developed via transition-metal catalyzed or transition-metal-free reactions, and direct functionalization at C-3 position for synthesis of ester functional groups was also extremely attractive. Based on our studies toward synthesis of 3-indolecarboxylates, the recent developments of synthesis of 3-indolecarboxylates by different synthetic methods in view of the types of substrates are reviewed.
Key words: 3-indolecarboxylate, metal-catalyzed cyclization, C—H functionalization, transition metal-free reaction, recent development


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