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Asymmetric one-carbon ring expansion of diverse N-heterocycles via copper-catalyzed diyne cyclization.


ABSTRACT: One-carbon ring expansion reaction of N-heterocycles has gained particular attention in the past decade because this method allows for the conversion of readily available N-heterocycles into potentially useful complex ring-expanded N-heterocycles, which are inaccessible by traditional methods. However, the catalytic asymmetric variant of this reaction has been rarely reported to date. Herein, we disclose an enantioselective one-carbon ring expansion reaction through chiral copper-catalyzed diyne cyclization, leading to the practical, atom-economic and divergent assembly of an array of valuable chiral N-heterocycles bearing a quaternary stereocenter in generally good to excellent yields with excellent enantioselectivities (up to >99% ee). This protocol represents the first example of asymme

SUBMITTER: Li FS 

PROVIDER: S-EPMC11463259 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature