摘要：

Inspired by the ubiquitous prevalence of 3-hydroxyoxindoles in natural products and pharmaceuticals, we herein disclose a direct and practical transition-metal-free asymmetric hydroxylation using commercially available Davis enantiopure oxaziridines as efficient oxidants, expeditiously affording an array of medicinally active 3-functionalized 3-hydroxy-2-oxindoles bearing quaternary stereocenters. The protocol features cheap reactants, ease of operation, scalability, and good functional-group tolerance and efficient formal synthesis of natural products.

展开