Microwave Promoted Simple, Efficient and Regioselective Synthesis of Trisubstituted Imidazo[1,2-a]benzimidazoles on Soluble Support

作者：Chen Li Hsun; Hsiao Ya Shan; Yellol Gorakh S; Sun Chung Ming^*

来源：ACS Combinatorial Science, 2011, 13(2): 112-119.

DOI：10.1021/co1000037

• microwave-assisted
• polymer-supported
• amino benzimidazoles
• biologically interesting

An efficient microwave-assisted and soluble polymer-supported synthesis of medicinally important imidazole-fused benzimidazoles has been developed. The protocol involves the rapid condensation of polymer-bound amino benzimidazoles with various alpha-bromoke-tones and subsequent in, situ intramolecular cyclization under microwave irradiation resulting in a one pot synthesis of imidazole interlacing benzimidazole polymer conjugates. The condensed product was obtained with excellent regioselectivity. The biologically interesting imidazo [1,2-a]benzimidazoles was released from polymer support at ambient temperature. Diversity in the triheterocyclic nucleus was achieved by the different substitutions at its 2, 3, and 9 positions. The new protocol has the advantages of short reaction time, easy workup process, excellent yields, reduced environmental impact, wide substrate scope and convenient procedure.

• 出版日期2011-4