Synfacts 2011(1): 0075-0075  
DOI: 10.1055/s-0030-1259114
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart ˙ New York

Pd-Ligand Controlled Cyclization for the Preparation of Heteroaromatics

Contributor(s):Paul Knochel, Andreas K. Steib
D. Tsvelikhovsky, S. L. Buchwald*
Massachusetts Institute of Technology, Cambridge, USA
Synthesis of Heterocycles via Pd-Ligand Controlled Cyclization of 2-Chloro-N-(2-vinyl)aniline: Preparation of Carbazoles, Indoles, Dibenzazepines and Acridines
J. Am. Chem. Soc.  2010,  132:  14048-14051  
Further Information

Publication History

Publication Date:
21 December 2010 (online)


Significance

Various vinyl diphenylamine intermediates are selectively cyclized to the corresponding five-, six- or seven-membered hetero­aromatics. The regioselectivity of these palladium-catalyzed cyclizations is almost exclusively directed by the used ligand.

Comment

By using 2-bromostyrene and 2-chloroaniline derivatives in this palladium-catalyzed ­reaction with DavePhos as ligand, a direct one-pot synthesis was achieved, furnishing 5H-diazepines in good to excellent yields.