- An Improved Process for the Enantioselective Synthesis of HCV NS5A Inhibitor Elbasvir (MK-8742) Chiral Amine Intermediate
-
Abstract: Large-scale enantioselective synthesis of the chiral amine unit of HCV NS5A inhibitor Elbasvir has been accomplished in six steps, with 55% overall yield. The process includes a highly enantioselective reduction of the NH imine using R-(+)-diphe
- Chapala, Vijaya Lakshmi,Katari, Naresh Kumar,Kerru, Nagaraju,Malavattu, Giri Prasad,Marisetti, Vishnu Murthy,Reddy, Pedavenkatagari Narayana
-
p. 932 - 938
(2021/06/26)
-
- PROCESS FOR PREPARING SUBSTITUTED INDOLE COMPOUNDS
-
The present invention is directed to a process for preparing Substituted Indole Compounds of Formula (I): wherein R1, R2, R3 and R4 are as defined herein. These indole compounds are useful as synthetic intermediates for making inhibitors of HCV NS5A.
- -
-
-
- Hepatitis C virus inhibitor and application thereof
-
The invention relates to a hepatitis C virus inhibitor and application thereof, and particularly discloses a compound which can be used as a hepatitis C virus and is as shown in a formula (I), or optical isomer, pharmaceutically acceptable salt, hydrate or solvate thereof, which can be used for treating hepatitis C virus (HCV) infection or hepatitis C diseases, or used as a hepatitis C virus nonstructural 5A (NS5A) protein inhibitor.
- -
-
Paragraph 0239-0242; 0245; 0246
(2018/01/13)
-
- PROCESS FOR PREPARING TETRACYCLIC HETEROCYCLE COMPOUNDS
-
The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
- -
-
Page/Page column 29; 30
(2015/05/19)
-
- Enantioselective synthesis of an HCV NS5a antagonist
-
A concise, enantioselective synthesis of the HCV NS5a inhibitor MK-8742 (1) is reported. The features of the synthesis include a highly enantioselective transfer hydrogenation of an NH imine and a dynamic diastereoselective transformation. The synthesis of this complex target requires simple starting materials and nine linear steps for completion.
- 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
-
supporting information
p. 2310 - 2313
(2014/05/20)
-
- An improved synthesis of hydroxy aryl ketones by fries rearrangement with methanesulfonic acid/methanesulfonic anhydride
-
Methanesulfonic acid treated with methanesulfonic anhydride effectively mediates the Fries rearrangement of aryl esters to give hydroxy aryl ketones with high yields. Georg Thieme Verlag Stuttgart · New York.
- Jeon, Ingyu,Mangion, Ian K.
-
experimental part
p. 1927 - 1930
(2012/10/08)
-