Catalytic Asymmetric [3+3] Cycloaddition of Azomethine Ylides with C3‐Substituted 2‐Indolylmethanols

The first catalytic asymmetric [3+3] cycloaddition of azomethine ylides with C3‐substituted 2‐indolylmethanols has been established, leading to diastereo‐ and enantioselective construction of a tetrahydropyrimido[1,6‐a]indole framework (up to 91% yield, >95:5 dr, 98:2 er). This reaction also represents a new type of catalytic enantioselective [3+3] cycloaddition using azomethine ylides. magnified image