Pd-Catalyzed Asymmetric Hydrogenation of Unprotected Indoles Activated by Brønsted Acids
Journal of the American Chemical Society2010Vol. 132(26), pp. 8909–8911
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Abstract
The first highly enantioselective hydrogenation of simple indoles was developed with a Brønsted acid as an activator to form the iminium intermediate in situ, which was hydrogenated using Pd(OCOCF(3))(2)/(R)-H8-BINAP catalyst system with up to 96% ee. The present method provides an efficient route to enantioenriched 2-substituted and 2,3-disubstituted indolines.
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