Application of New Organometallic Bases in the functionalization of nitriles of pharmaceutical interest

• Grant number: 12/13740-0
• Support Opportunities: Scholarships in Brazil - Doctorate
• Start date: October 01, 2012
• End date: July 31, 2016
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Giuliano Cesar Clososki
• Grantee: Fernanda Moraes dos Santos
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Associated research grant: 08/04762-4 - New synthetic methods for the preparation of bioactive compounds, AP.JP

Abstract

Zinc and Magnesium Organometallic bases complexed with lithium chloride were recently introduced in the literature and show great potential in the functionalization of several aromatic rings and heterocyclic. However, their reactivity towards important substrates has not yet been properly studied. This is the case of nitriles, which, although being a large and wide field of applications in organic synthesis, have received little attention from researchers working in the area. Thus, the main aim of this project is to develop methodologies for the preparation of highly functionalized nitriles and can be applied to the synthesis of bioactive molecules.In order to demonstrate the importance of the synthetic methodology, we intend to apply these in the synthesis or structural modification of bioactive molecules, such as venlafaxine, an antidepressant, and pyrimethamine, a substance that has been used to treat malaria. Moreover, the novel nitriles to be synthesized in this project could be tested by groups of the Faculty of Pharmaceutical Sciences of Ribeirão Preto - USP active in the biological evaluation of natural and synthetic substances.The proposals here presented are part of the project "Development of New Synthetic Methods Aimed at Preparation of Bioactive Molecules", approved by FAPESP through the Young Researcher modality with the objective of gather research groups that work with modern themes and with international integration.

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)

DOS SANTOS, FERNANDA M.; BATISTA, JOAO H. C.; VESSECCHI, RICARDO; CLOSOSKI, GIULIANO C.. Directed Functionalization of Cyano-Substituted Furans and Thiophenes with TMPMgCl center dot LiCl. Synlett, v. 26, n. 20, p. 2795-2800, DEC 2015. (13/04766-8, 12/13740-0, 14/23604-1)

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

SANTOS, Fernanda Moraes dos. Directed functionalization of aromatic and heteroaromatic nitriles using the base TMPMgCloLiCl. 2016. Doctoral Thesis - Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto (PCARP/BC) Ribeirão Preto.