Amidst interest in miniaturization of industrial and environmental footprints, the application of continuous flow in the synthesis of active pharmaceutical ingredients (API) is gaining attention. The advantages of continuous flow synthesis include the ability to telescope multistep syntheses, withstand high reaction temperatures and pressures, and enhance mixing, heat, and mass transfer. This presentation will describe the preparation of dolutegravir via a flow process. Dolutegravir is an HIV-integrase inhibitor approved for combination therapy, and functions by binding to the active site of the virus enzyme and blocking the transfer of viral DNA strands. Our results demonstrate a new and improved flow synthesis of dolutegravir in 7-steps from commercially available starting materials.

Flow synthesis of dolutegravir: Translating batch processes into flow

256th National Meeting (2018)

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