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Catalytic asymmetric construction of chiral indole‐fused rings has become an important issue in the chemical community because of the significance of such scaffolds. In this work, we have accomplished the first catalytic asymmetric (4+2) and (4+3) cycloadditions of 2,3‐indolyldimethanols by using indoles and 2‐naphthols as suitable reaction partners under the catalysis of chiral phosphoric acids, constructing enantioenriched indole‐fused six‐membered and seven‐membered rings in high yields with excellent enantioselectivities. In addition, this approach is used to realize the first enantioselective construction of challenging tetrahydroindolocarbazole scaffolds, which are found to show promising anticancer activity. More importantly, theoretical calculations of the reaction pathways and activation mode offer an in‐depth understanding of this class of indolylmethanols. This work not only settles the challenges in realizing catalytic asymmetric cycloadditions of indolyldimethanols but also provides a powerful strategy for the construction of enantioenriched indole‐fused rings.

A new chelation-controlled hydrofuranization of unactivated olefins with α-alkynyl arylols is reported for the first time, and used to produce a wide range of C3-alkylated benzofurans with generally good yields under mild conditions.

Developingi ndolyldimethanols … …asfour-carbon platform molecules for enantioselective cycloadditions is like climbing ahigher peak of the mountain:full of challenges but exciting.Intheir Research Article (e202305450), Shao-Fei Ni, WeiT an, Feng Shi et al. describe catalytic asymmetric (4+ +n) cycloadditions of indolyldimethanols,l eading to the construction of enantioenriched indole-fused rings.