Synthesis of Highly Substituted Pyrrolidines via Double Michael Addition Reaction and its Anti-Microbial Activity

The synthesis of Nitrogen base heterocycles particularly highly substituted pyrrolidines are very important skeleton of many biologically active molecules1 including natural and non-natural substances. The synthesis of functionalized pyrrolidines persists to attract interest, both for their synthetic challenges,2 and also their value in synthetic chemistry3 and their diverse biological activity.4 The present work includes the synthesis of highly substituted pyrrolidines through double Michael addition reaction of acetylene carboxylate with substituted malonate and amine in one pot results into the cyclisation. This methodology gives substitution pattern on 2, 2, 3,3,5-position of the pyrrolidines Scheme 1 and 3. This strategy is very simple and efficient to have highly substituted nitrogen containing heterocycle as pyrrolidines.