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Flow chemistry as enabling technology in the synthesis of...

Titel: «Flow chemistry as enabling technology in the synthesis of Entresto» - Paolo Filliponi, Novartis Pharma AG, Novartis campus, 4056 Basel, Switzerland paolo.filipponi@novartis.com

LCZ696 (Entresto) is an innovative heart disease medicine which exploits the pharmacological benefits of two drug substances, sacubitril and valsartan, combined together in a supramolecularcrystalline complex. While valsartan has been an established API since many years, a commercial process for the large-scale manufacturing of sacubitril had to be developed. The application of flow chemistry technology allowed the assembly of key molecular elements in sacubitril, achieving high quality and productivity standards. The drivers for the implementation of a continuous process on manufacturing scale will be discussed, and an overview of the challenges faced, and tasks accomplished in the journey from the proof-of-principle to the full development will be provided.

[1] Kleinbeck, F. et al., J. Org. Chem. 2020, 85, 6844-6853.

 

 

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