The Application of a Continuous Grignard Reaction in the Preparation of Fluconazole

    • Sudha Korwar
    • Somi Amir
    • Perrer N. Tosso
    • Bimbisar K. Desai
    • Caleb J. Kong
    • Swara Fadnis
    • Nakul S. Telang
    • Saeed Ahmad
    • Thomas D. Roper
    • B. Frank Gupton*
    • Department of Chemistry and Department of Chemical and Life Science, Engineering, Virginia Commonwealth University, 601 W. Main St., R ichmond, VA 23220, USA

    The application of continuous methods in the synthesis of active pharmaceutical ingredients continues to receive significant attention in the academic as well as the industrial research communities. One of the major advantages of continuous methods is the ability to safely access kinetic synthons as well as highly reactive reagents that are typically unavailable through traditional batch methods. In this work, we report the high‐yielding, clean formation of an aryl‐turbo Grignard and its selective addition to a highly‐enolizable 1,3‐dichloroacetone, for the continuous synthesis of a key intermediate for fluconazole, a widely‐prescribed anti‐fungal agent. In addition, process optimization of the final API was also carried out to arrive at a semi‐continuous method to this essential medicine.

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