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Selective aromatic functionalization: Methodological Studies and new applications in the synthesis of BIOATIVE compounds

Grant number: 18/14150-8
Support type:Regular Research Grants
Duration: September 01, 2018 - August 31, 2020
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Principal Investigator:Giuliano Cesar Clososki
Grantee:Giuliano Cesar Clososki
Home Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil


In the present project we intend to study the potential of organometallic reagents in the development of methodologies for selective functionalization of aromatic and heterocyclic substrates of great scientific and technological interest, mainly for Medicinal Chemistry. In this sense, directed metalation or halogen/metal exchange reactions in a series of aryl nitriles, quinolines, indolizines and quinoxalines, among other targets that may be of interest in the course of the project should allow the isolation of new highly functionalized aromatic and heterocyclic compounds. With the aim to better understand, rationalize and plan regioselective metalation reactions, computational chemistry tools will be used in the structural evaluation of all synthetic targets. Finally, in order to demonstrate the synthetic importance of the developed methodologies, applications in the preparation or structural modification of substances of medicinal interest, such as quinazolines and quinolines with potential antitumor activity, will be carried out. (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)
DE MELLO, MURILO B. M.; DE OLIVEIRA, ANTONIO A. F.; DE OLIVEIRA, CAROLINE L.; ULTRAMARI, MARIAH A.; GAETA, FERNANDO H. S.; MASCARELLO, ALESSANDRA; GUIMARAES, CRISTIANO R. W.; DE FREITAS, MILLER N.; CUNHA, CARLOS E.; LOURENCO, TIAGO C.; FERREIRA, FERNANDEZ P.; LOPES, JOAO L. C.; CLOSOSKI, GIULIANO C. Characterization and in silico Mutagenic Assessment of a New Betahistine Degradation Impurity. Journal of the Brazilian Chemical Society, v. 30, n. 7, p. 1415-1424, JUL 2019. Web of Science Citations: 0.
NISHIMURA, RODOLFO H. V.; VAZ, ARTUR DE L. L.; BOZZINI, LEANDRO A.; MURIE, VALTER E.; CLOSOSKI, GIULIANO C. Recent applications of magnesium- and Zinc-TMP amides in the synthesis of bioactive targets. Tetrahedron, v. 75, n. 4, p. 464-474, JAN 25 2019. Web of Science Citations: 1.

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