Polyfunctional heterocycles in drug discovery: diversity-oriented synthesis and chemico-physical analysis
Jun. 8, 2018 16:00 - 17:00
MI Bldg.LargeConferenceRoom 2F
Department of Chemistry, University of Tokyo
Diversity-oriented synthesis is emerging as a powerful tool in drug discovery due to its ability to generate a large number of compounds with high structural diversity in few steps. In this context, we developed a Ti(IV)-promoted three-component reaction of aromatic heterocycles, aldehydes, and active methylene compounds to afford polyfunctionalized heterocycles of biological interest . The experimental procedure was optimized by studying the reaction mechanism . The stereochemical stability of the products was also investigated by HPLC and NMR spectroscopy in view of their use as fragments in a fragment-based drug discovery approach .
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