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Organocatalytic insertion reactions for drug discovery

Grant number: 13/50312-9
Support type:Regular Research Grants
Duration: October 01, 2013 - September 30, 2014
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Cooperation agreement: Ohio State University
Principal Investigator:Antonio Carlos Bender Burtoloso
Grantee:Antonio Carlos Bender Burtoloso
Principal investigator abroad: Anita Elaine Mattson
Institution abroad: Ohio State University, Columbus, United States
Home Institution: Instituto de Química de São Carlos (IQSC). Universidade de São Paulo (USP). São Carlos , SP, Brazil
Associated research grant:12/04685-5 - New synthetic methodologies for the construction of pyrrolidine, piperidine and indolizidine systems, AP.R


A comprehensive research program with the long-term goal of discovering sustainable methods for drug target synthesis is proposed. Specifically, organocatalytic insertion reactions will be investigated. En route to realizing this goal, the objectives of this proposed research agenda include (i) exploring urea and phosphoric acid derivatives as catalysts for N-H and O-H insertion reactions of diazo compounds and (ii) applying innovative organocatalytic insertion reactions toward the syntheses of active pharmaceutical ingredients. The specific aims included in this proposed research plan are: 1) Study the activation of diazo compounds for insertion reactions with chiral urea catalysis (Mattson Laboratories - OSU), 2) Investigate the activation of diazo compounds for insertion reactions with chiral phosphoric acid-derived catalysis (Burtoloso Laboratories - USP) and 3) Apply new methods organocatalytic insertion methods toward the enantioselective syntheses of durg targets, including bupropion, duloxetine and fluoxetine (Burtoloso and Mattson Laboratories). (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)
BERNARDIM, BARBARA; COUCH, ERICA D.; HARDMAN-BALDWIN, ANDREA M.; BURTOLOSO, ANTONIO C. B.; MATTSON, ANITA E. Divergent Roles of Urea and Phosphoric Acid Derived Catalysts in Reactions of Diazo Compounds. SYNTHESIS-STUTTGART, v. 48, n. 5, p. 677-686, MAR 2016. Web of Science Citations: 11.

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