Development of Heteroaryl Compounds Targeting at Aromatase for Cancer Therapy

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Northern Kentucky University
Heteroaryl compounds are valuable building blocks in medicinal chemistry and chemical industry. A palladium-catalyzed direct αC(sp3) heteroarylation of ketones under microwave irradiation was performed to synthesize isocoumarin derivatives. The optimized reaction conditions are as follows: 1.1 equivalents of ketone, 1 equivalent of heteroaryl halide, 2.4 equivalents of NaOtBu, XPhos Pd Gen 4 catalyst, toluene, MW 1300 C for 10 min. The final product was purified by medium pressure liquid chromatography (MPLC) and characterized by nuclear magnetic resonance (NMR). This study provided insightful information for the development of bioactive heteroaryl compounds
2020 Celebration of Student Research and Creativity presentation
Aromatase, Cancer Treatment, Ketones