The first total synthesis of (+)-gliocladin B is described. Our concise and enantioselective synthesis takes advantage of a new regioselective Friedel-Crafts-based strategy to provide an efficient multigram-scale access to the C3-(3'-indolyl)hexahydropyrroloindole substructure, a molecular foundation present in a significant subset of epipolythiodiketopiperazine natural alkaloids. Our first-gen...

Gastro-intestinal (GI) toxicity is the common adverse effect which has been associated with most of NSAIDs available in the market. So the search for new therapeutic agents with high margin of safety and freedom from normally associated GI toxic effects has been a priority of pharmacologists and pharmaceutical industries. There are virtually limitless series of structurally novel heterocyclic c...