- An Improved Process for the Enantioselective Synthesis of HCV NS5A Inhibitor Elbasvir (MK-8742) Chiral Amine Intermediate
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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
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p. 932 - 938
(2021/06/26)
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- PROCESS FOR PREPARING SUBSTITUTED INDOLE COMPOUNDS
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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.
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- Hepatitis C virus inhibitor and application thereof
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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.
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- PROCESS FOR PREPARING TETRACYCLIC HETEROCYCLE COMPOUNDS
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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).
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- Enantioselective synthesis of an HCV NS5a antagonist
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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
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p. 2310 - 2313
(2014/05/20)
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- Asymmetric synthesis of cyclic indole aminals via 1,3-stereoinduction
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A general and efficient asymmetric synthesis of cyclic indoline aminals was developed with a high level of 1,3-stereoinduction through a dynamic crystallization-driven condensation. Dehydrogenation of the indoline aminals with potassium permanganate produced the corresponding cyclic indole aminals in high yields and excellent enantioselectivities. This general methodology was successfully applied to the synthesis of a wide variety of chiral cyclic indoline aminals and indole aminals with aromatic and aliphatic functional groups.
- Li, Hongmei,Chen, Cheng-Yi,Nguyen, Hoa,Cohen, Ryan,Maligres, Peter E.,Yasuda, Nobuyoshi,Mangion, Ian,Zavialov, Ilia,Reibarkh, Mikhail,Chung, John Y. L.
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p. 8533 - 8540
(2015/01/08)
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