Organocatalytic enantioselective synthesis of C-N atropisomers formal C-O bond amination.

Compared with well-developed construction of C-C atropisomers, the synthesis of C-N atropisomers remains in its infancy, which is recognized as both appealing and challenging. Herein, we achieved the first organocatalyzed asymmetric synthesis of C-N atropisomers by formal C-O amination. With the aid of a suitable acid, 3-alkynyl-3-hydroxyisoindolinones reacted smoothly with 1-methylnaphthalen-2-ols to afford a wide range of atropisomers by selective formation of the C-N axis.