Multicatalysis for the synthesis of original endoperoxides for antimalarial purposes

International audienceDue to the recent scientific progress in the development of anti-malarial compounds, new drugs have reached the market. However, the cost of some of these treatments continues to be an important problem for developing countries, where the number of cases reached 216 million in 2016, according to the World Health Organization [1].Many anti-malarial compounds have been developed, with artemisin derivatives being among the most effective. The peroxide function present in these molecules is showed to be an important moiety for their bioactivity [2] against Plasmodium falciparum, the parasite responsible for the disease.Taking this context into account, the main objective studied in this project is the synthesis and applications of catalytic methods for an efficient and inexpensive preparation of new polycyclic α-nitrogenous endoperoxides, which have a significant potential as active molecules against malaria [3, 4, 5, 6].[1] World Health Organization, June 11th 2018: http://www.who.int/news-room/fact-sheets/detail/malaria[2] C. Madelaine, Y. Six, O. Buriez, Angew. Chem. Int. Ed. 2007, 46, 8046-8049[3] L. Banfi, A. Basso, V. Cerulli, G. Guanti, and R. Riva. J. Org. Chem. 2008, 73, 1608-1611[4] C. Chen, P. Kattanguru, O. A. Tomashenko, R. Karpowicz, G. Siemiaszko, A. Bhattacharya, V. Calasans and Y. Six. Org. Biomol. Chem. 2017, 15, 5364-5372[5] F. Liu, D. Ding, Heterocycles, 2015, 91, 4.[6] A. Bledé-Font, Tetrahedron Lett. 1980, 21, 2443-2446