A scalable synthesis to an advanced intermediate 7a (+/-)  in the synthesis of 8 , a potent BACE inhibitor, has been developed and demonstrated on kilogram scale. An improved and scalable route to 5  will be discussed. The diastereoselective reduction of 5  with L-selectride, and the Bucherer-Bergs cyclization to 7a (+/-)  will also be discussed.

Process development towards a scalable synthesis of a potent BACE inhibitor

248th National Meeting (2014)

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