|Date and Time||2018年06月08日 16:00 - 17:00|
|Venue||MI Bldg.LargeConferenceRoom 2F|
|Affiliation||Department of Chemistry, University of Tokyo|
|Poster||click here to download(PDF)|
|Title||Polyfunctional heterocycles in drug discovery: diversity-oriented synthesis and chemico-physical analysis|
|Summary||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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