Highly regio-and enantioselective synthesis of chiral polysubstituted 2H-pyrroles
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摘要:
As one of the most important five-member heterocyclic aromatic rings,pyrrole is widely distributed in numerous natural products and pharmaceutical agents.Asymmetric dearomatization of pyrroles is very attractive in organic synthesis given the fact that highly functionalized chiral pyrrolines and pyrrolidines could be easily accessed from the readily available pyrroles.However,the reported asymmetric dearomatization reactions of pyrroles are limited to transition-metal-catalyzed [4+3] cycloaddition and hydrogenation reactions.The enantioselective intermolecular alkylative dearomatization of pyrroles is rare and challenging due to multiple selectivity issues including the chemoselectivity (C2&N1),regioselectivity (C2&C4,C2&C5) and enantioselectivity (Scheme 1) [1].