Key Laboratory of Natural Medicines, Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Molecules. 2022 Dec 17;27(24):9008. doi: 10.3390/molecules27249008.
The construction of an N-C chiral axis for N-aryl indole derivatives is meaningful as they widely exist in functionalized molecules. This work provides a novel method for this purpose via amination of amino acid derivatives at the C2 position of the indole and chiral center induced chiral axis formation. The protocol of this transformation is easily accessible, not requiring metal or an organic chiral catalyst, endowing this method with great potential in the construction of axis chiral -aryl indoles.
构建 N-芳基吲哚衍生物的 N-C 手性轴具有重要意义，因为它们广泛存在于功能化分子中。本工作通过在吲哚的 C2 位和手性中心上进行氨基酸衍生物的氨化反应，提供了一种新颖的方法来实现这一目标，从而诱导手性轴的形成。该转化的方案易于实现，不需要金属或有机手性催化剂，这使得该方法在手性轴芳基吲哚的构建中具有很大的潜力。
