The design of experiments (DoE) in optimization of an aerobic flow Pd-catalyzed oxidation of alcohol towards an important aldehyde precursor in the synthesis of phosphatidylinositide 3-kinase inhibitor (CPL302415)

    • Stanisław Michałeka,b
    • Lidia Gurba-Bryśkiewicza
    • Wioleta Maruszaka
    • Marcin Zagozdaa
    • Anna M. Maja
    • Zbigniew Ochalb
    • Krzysztof Dubiela
    • Maciej Wieczoreka
    • aCelon Pharma S.A., Ul. Marymoncka 15, 05-152 Kazuń Nowy, Poland
    • bFaculty of Chemistry, Warsaw University of Technology, Ul. Noakowskiego 3, 00-664 Warsaw, Poland

    Herein, we describe the development of a green, scalable flow Pd-catalyzed aerobic oxidation for the key step in the synthesis of CPL302415, which is a new PI3Kδ inhibitor. Applying this environmental-friendly, sustainable catalytic oxidation we significantly increased product yield (up to 84%) and by eliminating of workup step, we improved the waste index and E factor (up to 0.13) in comparison with the stoichiometric synthesis. The process was optimized by using the DoE approach.

    Read the publication that featured this abstract

    Get in touch

    For more information on flow chemistry systems and services please use the contact methods below.

    Call us on +44 (0)1284 728659 or Email us