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
Read the publication that featured this abstractHerein, 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.
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