Development of the telescoped flow Pd-catalyzed aerobic alcohol oxidation/reductive amination sequence in the synthesis of new phosphatidylinositide 3-kinase inhibitor (CPL302415)

Michałek et al. present an efficient two-step continuous flow synthesis of CPL302415 (3), a novel phosphatidylinositide 3-kinase delta (PI3Kδ) inhibitor under investigation for the treatment of systemic lupus erythematosus. The process begins with a palladium-catalyzed aerobic oxidation to form aldehyde intermediate 2, followed by a reductive amination to yield the final API. This flow-based method was optimized using a Design of Experiments (DoE) approach and successfully applied to the synthesis of additional biologically active CPL302415 derivatives. The work highlights the scalability and versatility of flow chemistry in the development of kinase inhibitors for autoimmune diseases.

• Michałek, S
• Maj, AM
• Gurba-Bryśkiewicz, L
• Maruszak, W
• Wiśniewski, K
• Zagozda, M
• Stypik, M
• Dubiel, K
• Wieczorek, M

• Celon Pharma S.A. ul. Marymoncka 15 05-152 Kazuń Nowy Poland

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