Abstract
The scalable route to PF-07059013 (3), a non-covalent modulator of hemoglobin for the treatment of sickle cell disease, is discussed. Optimization of the discovery route is presented, examining bond connections, late-stage Buchwald–Hartwig C–O coupling, and palladium content reduction strategies. The first process chemistry route to deliver 11 kg of the final API is also discussed.
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