Copper(I)-Catalyzed Kinetic Resolution of N‑Sulfonylaziridines with Indoles: Efficient Construction of Pyrroloindolines

The first Lewis acid catalyzed [3 + 2] annulation of indoles and 2-aryl-N-tosylaziridines was realized by using copper­(I)/chiral diphosphine complexes as a catalyst. With this method, a variety of uniquely substituted chiral pyrroloindolines bearing multiple contiguous stereogenic centers were facilely accessed in a straightforward, high-yielding, and highly stereoselective way under mild conditions.