Design and synthesis of novel enantiomerically enriched morpholino [4, 3–a] benzimidazole derivatives as potential bioactive agents

A series of chiral morpholino [4, 3-a] benzimidazole derivatives were synthesized effectively from (S)-(-)-2-(α-hydroxyethyl)-benzimidazole and phenacyl bromide derivatives using an efficient synthetic protocol in good yields and moderate diastereoselectivities. The substrate controlled diastereoselective route makes available structurally attractive morpholine-fused benzimidazole derivatives with two chiral centers in enantiomerically enriched forms. The preliminary biological evaluation shows scope for potential applications.