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Organocuprate Mediated Synthesis of 2-Alkyl-substituted Thiochromanones

Undergraduate #168
Discipline: Chemistry and Chemical Sciences
Subcategory: Chemistry (not Biochemistry)
Session: 1

Shekinah Bass - Winston-Salem State University
Co-Author(s): Tania Bellinger, Winston Salem State University, Winston Salem, NC ; Fenghai Guo, Winston Salem State University, Winston Salem, NC



Thiochromones undergo conjugate addition reactions with alkylcuprates to afford thiochromanones (2-alkyl substituted thiochroman-4-ones), providing an efficient synthetic approach to privileged sulfur-containing structural motifs and valuable precursor for many pharmaceuticals. Excellent yields of 2-alkyl substituted thiochroman-4-ones can be attained with lithium dialkylcuprates, lithium alkylcyanocuprates and Grignard reagents with copper catalysis. This method provides a rapid entry to a variety of thiochromanones in excellent yields (up to 88%). The use of commercially available or easily prepared organometallic reagents will expedite the synthesis of a large library of thiochromanone and derivatives for further synthetic applications and biological studies.

Funder Acknowledgement(s): NSF HBCU-UP research initiation award (award no. 1600987).

Faculty Advisor: Fenghai Guo, guof@wssu.edu

Role: I developed the organocuprate mediated 1-4 conjugate addition of Grignard Reagents to thiochromones. Investigated the effect of alkyl groups and different types of copper salts and solvent effects on the substituted thiochromone. Both substituted and non-substituted thiochromones were investigated. I also synthesized a variety of bioactive 2-substituted thiochromanones. Thiochromanones are key intermediates for bioactive products such as sulfoxides. Currently, I am working on making other bioactive products such as sulfoxides and sulfones. Recently I just published some of these results in a paper.

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This material is based upon work supported by the National Science Foundation (NSF) under Grant No. DUE-1930047. Any opinions, findings, interpretations, conclusions or recommendations expressed in this material are those of its authors and do not represent the views of the AAAS Board of Directors, the Council of AAAS, AAAS’ membership or the National Science Foundation.

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