Friday, 6 October 2006
South Ballroom (Binghamton Regency Hotel and Conference Center)
443

An Effective Procedure for the Preparation of N-Substituted (Aza)indoles and (Aza)benzimidazole

Zhongxing Zhang, Juliang Zhu, Zhiwei Yin, Nicholas A. Meanwell, John F. Kadow, and Tao Wang. Bristol-myers Squibb Pharmaceutical Research Institute, Wallingford, CT

N-Substituted (aza)indoles, as well as (aza)benzimidazole were prepared from ortho-methyl bromo pyridines or benzenes.  The procedure sequentially involved: a) condensation of a 2-methy or 2-amino l-bromo pyridine or benzene with N,N-dimethylformamide dimethyl acetal; b) microwaved palladium-mediated amination; c) in situ cyclization of the aniline with enamine or amidine moiety and elimination of dimethyl amine.

 

 


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