Organocatalytic Enantioselective Higher-Order Cycloadditions of In Situ Generated Amino Isobenzofulvenes

Angew Chem Int Ed Engl. 2018 Jan 26;57(5):1246-1250. doi: 10.1002/anie.201710694. Epub 2018 Jan 5.

Abstract

The [8+2] cycloaddition of indene-2-carbaldehydes and nitro olefins is described to provide benzonorbornene scaffolds in a highly peri-, diastereo-, and enantioselective fashion in the presence of a C2 -symmetric aminocatalyst. This reaction, which proceeds through a transient semi-aromatic amino isobenzofulvene, represents the first example of catalytic formation and transformation of these species. Quantum chemical calculations suggest a kinetically controlled stepwise mechanism where the stereochemistry is determined in the first bond-forming event. Beyond the useful [8+2] cycloadducts, [10+4] cycloadducts have been identified in silico as potential off-pathway intermediates.

Keywords: cycloaddition; enantioselectivity; fulvenes; organocatalysis; reaction mechanisms.

Publication types

  • Research Support, Non-U.S. Gov't