Evolution of the Manufacturing Route towards a Key Benzothiophen‐2‐yl‐Boronic Acid Building Block of Rogaratinib
Jörg Gries,
Johannes Platzek,
Holger Paulsen
Abstract:The evolution of the synthesis of a benzothiophene‐2‐yl‐boronic acid ‐ a key building block for the anti‐cancer agent Rogaratinib ‑ is reported from multi‐gram scale to industrialization. The pitfalls and learnings during process development are outlined, describing the optimization of the initial research synthesis route, investigation of an alternative approach based on a palladium‐catalyzed Newman‐Kwart rearrangement and finally changing the synthetic strategy from thiophene‐construction to benzene‐ring for… Show more
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