Synfacts 2006(8): 0774-0774  
DOI: 10.1055/s-2006-941979
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart · New York

Synthesis and Transformations of Fused Bicyclic Heteroaryl Borates

Contributor(s): Victor Snieckus, Bärbel Wittel
E. F. DiMauro*, J. R. Vitullo
Amgen Inc., Cambridge, USA
Further Information

Publication History

Publication Date:
21 July 2006 (online)

Significance

The synthesis of complex benzo[b]thiophenes, benzo[b]furans, and 2,6-disubstituted imidazo[1,2-a ]pyridines using a microwave-assisted, one-pot cyclization-Suzuki coupling approach is reported. The heterocycles were obtained in moderate to good yields depending on the substituent R1 by treatment of boronate precursors, which are prepared in advance, with 6-bromoquinazolin-2-amine, and α-bromoketone.