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Enantioselective Michael/Mannich Polycyclization Cascade of Indolyl Enones Catalyzed by Quinine-Derived Primary Amines


  • We thank the National Natural Science Foundation of China (20732006, 20821002, 21025209), the National Basic Research Program of China (973 Program 2010CB833300), and the Chinese Academy of Sciences for generous financial support.


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Three′s a crowd: The title reaction provides a tetracylic core bearing three chiral centers (see scheme; Ts=4-toluenesulfonyl) with excellent enantioselectivity and good diastereoselectivity. The reaction was used to efficiently construct the (+)-kreysiginine skeleton.