Improved Process for a Copper-Catalyzed C–N Coupling in the Synthesis of Verubecestat-Reference-Cited by-同舟云学术

Improved Process for a Copper-Catalyzed C–N Coupling in the Synthesis of Verubecestat

Published:2019-07-23 Issue:8 Volume:23 Page:1674-1678
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Phillips Eric M.¹^ORCID,Reibarkh Mikhail¹,Limanto John¹,Kieu Minh¹,Lekhal Azzeddine¹,Zewge Daniel¹

Affiliation:

1. Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.9b00192

Reference15 articles.

1. a Scott, J. D.; Stamford, A. W.; Gilbert, E. J.; Cumming, J. N.; Iserloh, U.; Misiaszek, J. A.; Li, G. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use. PCT Int. Appl., WO 2011/044181 A1, PCT/ US2010/051553, 2011.

2. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

3. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer’s disease patients

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

5. A Next Generation Synthesis of BACE1 Inhibitor Verubecestat (MK-8931)

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