Indole based alkaloids are well known in the literature for their diverse biological properties. Polysubstituted optically active tetrahydro-beta-carboline derivatives functionalized on C-1 position are the common structural motif in most of the indole based alkaloids as well as highly marketed drugs. The stereoselective Pictet-Spengler reaction is one of the currently most important synthetic techniques used for the preparation of these privileged tetrahydro-beta-carboline scaffolds. To date there are numerous research reports that have been published on the synthesis of the tetrahydro-beta-carboline scaffold both on solid phase as well as in solution phase. Moreover rapid growth has been observed for the enantioselective synthesis of tetrahydro-beta-carboline scaffold using chiral organocatalysts. In this book, efforts have been taken to shed light on the latest information available on different strategies to synthesize tetrahydro-beta-carboline both on solid phase and in solution phase during the last 20 years.
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