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Nine-Membered Benzofuran-Fused Heterocycles: Enantioselective Synthesis by Pd-Catalysis and Rearrangement via Transannular Bond Formation

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posted on 2017-10-17, 00:00 authored by Zi-Qiang Rong, Li-Cheng Yang, Song Liu, Zhaoyuan Yu, Ya-Nong Wang, Zher Yin Tan, Rui-Zhi Huang, Yu Lan, Yu Zhao
The first enantioselective formal [5+4] cycloaddition is realized under palladium catalysis to deliver benzofuran-fused nine-membered rings. These medium-sized heterocycles and derivatives undergo unique rearrangements induced by transannular bond formation, resulting in the production of two classes of densely substituted polycyclic heterocycles in excellent efficiency and stereoselectivity.

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