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- David A Thaisrivongs, William J Morris, Lushi Tan, Zhiguo J Song, Thomas W Lyons, Jacob H Waldman, John R Naber, Wenyong Chen, Lu Chen, Baoyun Zhang, and Jun Yang.
- Process Research and Development , Merck & Co., Inc. , P.O. Box 2000 , Rahway , New Jersey 07065 , United States.
- Org. Lett. 2018 Mar 16; 20 (6): 1568-1571.
AbstractThe development of a commercial manufacturing route to verubecestat (MK-8931) is described, highlights of which include the application of a continuous processing step to outcompete fast proton transfer in a Mannich-type ketimine addition, a copper-catalyzed amidation reaction, and an optimized guanidinylation procedure to form the key iminothiadiazine dioxide core.
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