Reported herein is a method for the construction of azepino[1,2‐a]indoles via an intramolecular aldehyde–alkyne metathesis of 1‐(5‐aryl‐4‐pentynyl)indole‐2‐carbaldehydes. This Sc(OTf)3‐catalyzed reaction has several remarkable features, such as ready accessibility of the starting materials, broad substrate scope, operational simplicity, and high yields. The practicality of the process and the synthetic potential of the products were demonstrated with an upscaling experiment and downstream synthetic derivatizations of the obtained products. We have also extended this methodology to synthesize a 6,7‐dihydropyrido[1,2‐a]indole derivative.

中文翻译：

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催化分子内醛-炔复分解方法制备 Azepino[1,2-a]吲哚


本文报道了一种通过 1-(5-芳基-4-戊炔基)吲哚-2-甲醛的分子内醛-炔复分解构建氮杂并[1,2-a]吲哚的方法。这种 Sc(OTf)3 催化反应具有几个显着的特点，例如起始材料易于获取、底物范围广泛、操作简单和产率高。通过放大实验和所得产品的下游合成衍生化证明了该工艺的实用性和产品的合成潜力。我们还扩展了这种方法来合成 6,7-二氢吡啶并[1,2-a]吲哚衍生物。