Elbasvir

CAT#: H510306

CAS#: 1370468-36-2

Description: Elbasvir, also known as MK-8742, is a HCV NS5A inhibitor, which is currently in phase 2b clinical trials as part of an all-oral, interferon-free regimen for the treatment of HCV infection. The NS5A protein plays a critical role in the replication of HCV and has been the focus of numerous research efforts over the past few years. NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays, making them attractive components for inclusion in all oral combination regimens.

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Synthetic Routes

Elbasvir - Synthetic Route 1

Elbasvir route01

Synthetic reference

Coburn, Craig A.; Meinke, Peter T.; Chang, Wei; Fandozzi, Christine M.; Graham, Donald J.; Hu, Bin; Huang, Qian; Kargman, Stacia; Kozlowski, Joseph; Liu, Rong; McCauley, John A.; Nomeir, Amin A.; Soll, Richard M.; Vacca, Joseph P.; Wang, Dahai; Wu, Hao; Zhong, Bin; Olsen, David B.; Ludmerer, Steven W. Discovery of MK-8742: An HCV NS5A inhibitor with broad genotype activity. ChemMedChem. Volume 8. Issue 12. Pages 1930-1940. Journal. (2013).

Elbasvir - Synthetic Route 2

Elbasvir route02

Synthetic reference

Li, Hongming; Belyk, Kevin M.; Yin, Jingjun; Chen, Qinghao; Hyde, Alan; Ji, Yining; Oliver, Steven; Tudge, Matthew T.; Campeau, Louis-Charles; Campos, Kevin R. Enantioselective Synthesis of Hemiaminals via Pd-Catalyzed C-N Coupling with Chiral Bisphosphine Mono-oxides. Journal of the American Chemical Society. Volume 137. Issue 43. Pages 13728-13731. Journal; Online Computer File. (2015).

Elbasvir - Synthetic Route 3

Elbasvir route03

Synthetic reference

Mangion, Ian K.; Chen, Cheng-yi; Li, Hongmei; Maligres, Peter; Chen, Yonggang; Christensen, Melodie; Cohen, Ryan; Jeon, Ingyu; Klapars, Artis; Krska, Shane; Nguyen, Hoa; Reamer, Robert A.; Sherry, Benjamin D.; Zavialov, Ilia. Enantioselective synthesis of an HCV NS5a antagonist. Organic Letters. Volume 16. Issue 9. Pages 2310-2313. Journal; Online Computer File. (2014).

Elbasvir - Synthetic Route 4

Elbasvir route04

Synthetic reference

Anon. A novel intermediate for the preparation of dimethyl ((2S,2'S)-((2S,2'S)-(((S)-6-phenyl-6H-benzo[5,6][1,3]oxazino[3,4-a]indole-3,10-diyl)bis(1H-imidazole-5,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-1,2-diyl))dicarbamate. IP.com Journal. Volume 16. Issue 8A. Pages 1-5. Journal; Patent. (2016).

Elbasvir - Synthetic Route 5

Elbasvir route05

Synthetic reference

Yin, Jingjun; Itoh, Tetsuji; Yin, Jianguo; Xiang, Bangping; Campos, Kevin R.; Kalinin, Alexei; Liu, Zhuqing; Christensen, Melodie Deniz; Belyk, Kevin; Varsolona, Richard J.; Brunskill, Andrew. Process for preparing substituted tetracyclic heterocycle compounds. Assignee Merck Sharp & Dohme Corp., USA. WO 2016196932. (2016).