Tying up loose ends: A copper(I)-catalyzed three-component reaction has been developed that leads to the formation of 2-(aminomethyl)indole derivatives. Water is the sole theoretical by-product in this reaction in which two CN bonds and one CC bond are formed. This route to the indole nucleus in combination with a palladium-catalyzed functionalization of a CH bond is also useful for the synthesis of polycyclic indoles (see scheme).
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Ohno et al. (2007) studied this question.
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