Synfacts 2009(10): 1156-1156  
DOI: 10.1055/s-0029-1217941
Organo- and Biocatalysis
© Georg Thieme Verlag Stuttgart ˙ New York

Intermolecular Addition of Indoles to Cyclic N-Acyliminium Ions

Contributor(s): Benjamin List, Kristina Zumbansen
E. A. Peterson, E. N. Jacobsen*
Harvard University, Cambridge, USA
Further Information

Publication History

Publication Date:
22 September 2009 (online)

Significance

A highly enantioselective intermolecular addition of indoles to cyclic N-acyliminium ions catalyzed by thiourea Schiff base 1 is presented. Electron-rich and electron-deficient indole nucleophiles are suitable substrates for this transformation. For electron-rich indoles TMSCl is used as an additive, whereas for the addition of electron-deficient indoles BCl3 turned out to be a more efficient additive. A catalytic cycle is proposed, where chlorolactam 2 is anticipated as the actual substrate in the alkylation.