Indole synthesis - something old, something new
Indole synthesis - something old, something new
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DOI：
10.1039/c2sc21185h
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发表时间：
2013-01-01
期刊：
影响因子：
8.4
通讯作者：
Moody, Christopher J.
中科院分区：
文献类型：
--
作者：
Inman, Martyn;Moody, Christopher J.
吲哚类化合物，既有天然存在的，也有合成的，具有广泛的生物活性。在它们的天然衍生物中出现了不寻常和复杂的分子结构。因此，这一重要的环系继续引起国际化学界的关注，并不断开发新的方法来构建这一一直相关的杂芳环。遗憾的是，许多方法经常从邻位取代的苯胺开始，从而极大地限制了起始材料的可用性。一种更一般的方法是从单官能化芳烃开始，如苯胺或卤苯，然后通过C-C或C-N键形成环化反应到未活化的C-H键。这些方法就是这一视角的主题。
Indoles, both naturally occurring and synthetic, exhibit wide-ranging biological activity. Unusual and complex molecular architectures occur among their natural derivatives. As a result, this important ring system continues to attract attention from the international chemical community, and new methodologies for the construction of this ever relevant heteroaromatic ring continue to be developed. Unfortunately, many methods frequently start from ortho-substituted anilines, thereby greatly restricting the availability of starting materials. A more general approach would start from a mono-functionalized arene such as an aniline or halobenzene, followed by cyclization with C-C or C-N bond formation to an unactivated C-H bond. Such methods are the subject of this perspective.