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Updated: Jul 12, 2026

Continuous Flow Chemistry: Reaction of Diphenyldiazomethane with p-Nitrobenzoic Acid
Published on: November 15, 2017
A concise and practical route to Gedatolisib via a continuous-flow Kumada coupling reaction
Jianhai Yang1,2, Jun Li1,2, Donghe Tian3
1Institute of Zhejiang University - Quzhou Quzhou Zhejiang 324000 China 0624959@zju.edu.cn nb23028@zju.edu.cn.
None:
A practical three-step route to Gedatolisib, a dual PI3K/mTOR inhibitor for breast cancer, has been developed, featuring a key continuous-flow iron-catalyzed Kumada coupling. This continuous-flow setup enhances heat and mass transfer, eliminates the need for noble metal catalysts and associated removal steps. This approach avoids hazardous reagents as well as high-boiling solvents, thereby improving both safety and scalability. The 100 gram scale synthesis affords Gedatolisib in 66% overall yield (98.9% purity), featuring mild conditions and crystallization-based purification, offering lower costs and better scalability for industrial production.
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