Catalytic asymmetric multicomponent 1,2-boronate rearrangements provide a practical approach for synthesizing highly valuable enantioenriched boronic esters. When applied to alkenyl or heteroaryl boronates, these reactions have relied mainly on transition-metal catalysis. Herein, we present an organocatalytic, Lewis base-catalyzed asymmetric multicomponent 1,2-boronate rearrangement, involving indoles, boronic esters, and Morita–Baylis–Hillman carbonates, leading to enantioenriched, highly substituted indole and indoline derivatives. Using cinchona alkaloid-based catalysts, high selectivity has been achieved, enabling expansion of the chemical space around pharmaceutically relevant indole and indoline derivatives.

中文翻译：

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有机催化与 1,2-硼酸盐重排的合并：Lewis 碱催化的不对称多组分反应


催化不对称多组分 1,2-硼酸盐重排为合成高价值的对映体富集硼酯提供了一种实用方法。当应用于烯基或杂芳基硼酸盐时，这些反应主要依赖于过渡金属催化。在此，我们提出了一种有机催化的 Lewis 碱催化的不对称多组分 1,2-硼酸盐重排，涉及吲哚、硼酯和 Morita-Baylis-Hillman 碳酸盐，导致对映体富集、高度取代的吲哚和吲哚啉衍生物。使用基于金鸡纳生物碱的催化剂，已经实现了高选择性，从而能够扩大围绕制药相关吲哚和吲哚啉衍生物的化学空间。