A small molecule BACE inhibitor with high molecular complexity was developed as a clinical candidate for the treatment of Alzheimer’s disease. In order to rapidly advance the candidate from discovery chemistry to the clinic, multi-kilogram quantities were required. Key challenges for kilogram production that required development included control of regioisomeric impurities, cryogenic lithiated sulfone addition to a sulfinimine, and ozonolysis.

Integration of discovery and process development to deliver a high complexity BACE inhibitor

256th National Meeting (2018)

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