Polyfunctional heterocycles in drug discovery: diversity-oriented synthesis and chemico-physical analysis
2018年6月8日 16:00 - 17:00
カテゴリー
セミナー
場所
神戸
会場
MI Bldg.LargeConferenceRoom 2F
スピーカー
Andrea Renzetti
所属
Department of Chemistry, University of Tokyo
ポスター
概要
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 [1]. The experimental procedure was optimized by studying the reaction mechanism [2]. 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 [3].
References
[1] A. Renzetti, E. Dardennes, A. Fontana, P. De Maria, J. Sapi, S. Gérard J. Org. Chem. 2008, 73, 6824.
[2] A. Marrone, A. Renzetti, P. De Maria, S. Gérard, J. Sapi, A. Fontana, N. Re Chem. Eur. J. 2009, 15, 11537.
[3] A. Renzetti, A. Di Crescenzo, F. Nie, A. D. Bond, S. Gérard, J. Sapi, A. Fontana, C. Villani Chirality 2015, 27, 779.
ホスト
Takamitsu Hosoya
