%0 Journal Article %A Tiwari, Pawankumar R. %A John, Marina E. %A Karnik, Anil V. %D 2018 %T Design and synthesis of novel enantiomerically enriched morpholino [4, 3–a] benzimidazole derivatives as potential bioactive agents %U https://tandf.figshare.com/articles/journal_contribution/Design_and_synthesis_of_novel_enantiomerically_enriched_morpholino_4_3_a_benzimidazole_derivatives_as_potential_bioactive_agents/7189511 %R 10.6084/m9.figshare.7189511.v1 %2 https://ndownloader.figshare.com/files/13238999 %K L-(+)-lactic acid %K chiral benzimidazole %K morpholine %K diastereoselective reductions %K intramolecular cyclization %X

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.

%I Taylor & Francis