• Organic letters · Nov 2016

    Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease.

    • David A Thaisrivongs, Steven P Miller, Carmela Molinaro, Qinghao Chen, Zhiguo J Song, Lushi Tan, Lu Chen, Wenyong Chen, Azzeddine Lekhal, Sarah K Pulicare, and Yanke Xu.
    • WuXi AppTec (Shanghai) Pharmaceutical Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
    • Org. Lett. 2016 Nov 18; 18 (22): 5780-5783.

    AbstractVerubecestat is an inhibitor of β-secretase being evaluated for the treatment of Alzheimer's disease. The first-generation route relies on an amide coupling with a functionalized aniline, the preparation of which introduces synthetic inefficiencies. The second-generation route replaces this with a copper-catalyzed C-N coupling, allowing for more direct access to the target. Other features of the new route include a diastereoselective Mannich-type addition into an Ellman sulfinyl ketimine and a late-stage guanidinylation.

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