Ruthenium-catalyzed site selective C-H activation reactions in heteroarenes

• Grant number: 16/24448-9
• Support Opportunities: Scholarships abroad - Research Internship - Doctorate
• Start date: May 01, 2017
• End date: February 28, 2018
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Flavio da Silva Emery
• Grantee: Fernando Fumagalli
• Supervisor: Lutz Ackermann
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Institution abroad: Göttingen University, Germany
• Associated to the scholarship: 15/06588-5 - Development of library of heterocyclic fragments based on new heteroaromatic cores, BP.DR

Abstract

The fast and efficient development of new drugs have been reached by using modern strategies as the Fragment-Based Drug Discovery (FBDD), which from a screened fragment with low potency, a lead compound is obtained by optimization process. For this, the heteroaromatics compounds highlight as good fragments because of their physicochemical and electronic proprieties. So far, our group has been working in the synthesis of new heteroaromatic cores. However, for further application at FBDD, this compounds need to have its chemical reactivity studied. In this context, this project aims to establish collaboration with the research group of Lutz Ackermann of Georg-August-University Göttingen, who has large experience at ruthenium-catalyzed site selective C-H activation reactions in arenes and heteroarenes. We propose to apply these modern synthetic methods to develop efficient strategies of functionalization of heteroaromatic cores with pyridone and pyridazone fused systems, as well to the 2,3-substituted furo[2,3-b]pyridine core. Furthermore, the internship allows the establishment of a permanent cooperation between the two institutions. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

FUMAGALLI, FERNANDO; WARRATZ, SVENJA; ZHANG, SHOU-KUN; ROGGE, TORBEN; ZHU, CUIJU; STUECKL, A. CLAUDIA; ACKERMANN, LUTZ. Arene-Ligand-Free Ruthenium(II/III) Manifold for meta-C-H Alkylation: Remote Purine Diversification. CHEMISTRY-A EUROPEAN JOURNAL, v. 24, n. 16, p. 3984-3988, MAR 15 2018. (16/24448-9)