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, PolandRead the publication that featured this abstract
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.
The Vapourtec R-Series is, quite simply, unrivalled for flow chemistry
- Flexible |
- Precise |
The R-Series is undoubtedly the most versatile, modular flow chemistry system available today.
The Vapourtec E-Series is the perfect introductory system for flow chemistry
- Robust |
- Easy to use |
The E-Series is a robust and affordable, entry level flow chemistry system designed for reliability and ease of use.