Isocoumarin compounds have found significant applications in vast variety of medicinal chemistry research due to their wide range of biological activities. This project focuses on substrate scope investigation and mechanism study of domino reactions which generate heteroaryl isocoumarins as potential anti-breast cancer drug candidates. A variety of ketones and heteroaryl halides were tested under optimized reaction conditions with assistance of microwave irradiation. Over a dozen of heteroaryl isocoumarins were successfully synthesized in efficient time with minimal waste produced. In addition, 18O-acetophenone introduced from phenylacetylene, H218O, MsOH, and CF3CH2OH was used to narrow possible mechanistic routes of domino reactions. Future analyses include HRMS and bioassay to confirm chemical structures and efficacy in aromatase inhibition of synthesized products, respectively.

Heteroaryl isocoumarins as potential aromatase inhibitors: Substrate scope investigation and mechanism study using 18O-acetophenone

2019 Spring National Meeting

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