The concurrent construction of 1,3-stereocenters remains a challenge. Herein, we report the development of stereoselective union of a point chiral center with allenyl axial chirality in 1,3-position by Pd-catalyzed asymmetric allenylic alkylation between racemic allenyl carbonates and indanone-derived β-ketoesters. Various target products bearing a broad range of functional groups were afforded in high yield (up to 99%) with excellent enantioselectivities (up to 98% ee) and good diastereoselectivities (up to 13:1 dr).
An efficient and environmentally friendly methodology for 3,3‐dichlorination and 2‐oxidation of indole derivatives is described. Using KI as promotor, MCl (M=K, Na) as chlorine source, and oxone as oxidant, the reaction proceeds smoothly affording various functionalized 3,3‐dichloro‐2‐oxindoles in moderate to excellent yields. This strategy can also be extended to 3‐substituted indoles. With a broad substrate scope, it is a practical approach to 3,3‐disubstituted‐2‐oxindoles.
The efficient squaramide-catalyzed asymmetric allylic alkylation of 4-aminopyrazolones with various MBH carbonates via different pathways has been described. This method provides access to a series of pyrazolone derivatives bearing a...
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