945686-46-4Relevant academic research and scientific papers
Synthesis method of Beclabuvir intermediate
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Paragraph 0029-0031, (2019/07/10)
The invention discloses a synthesis method of a Beclabuvir intermediate. According to the method, beta-methyl bromopropionate is used as a starting material, and a target product is then prepared through diazotization, asymmetric cyclopropanation, alkylat
The First Kilogram Synthesis of Beclabuvir, an HCV NS5B Polymerase Inhibitor
Bien, Jeffrey,Davulcu, Akin,Delmonte, Albert J.,Fraunhoffer, Kenneth J.,Gao, Zhinong,Hang, Chao,Hsiao, Yi,Hu, Wenhao,Katipally, Kishta,Littke, Adam,Pedro, Aghogho,Qiu, Yuping,Sandoval, Maria,Schild, Richard,Soltani, Michelle,Tedesco, Anthony,Vanyo, Dale,Vemishetti, Purushotham,Waltermire, Robert E.
, p. 1393 - 1408 (2018/09/06)
The process development and kilogram-scale synthesis of beclabuvir (BMS-791325, 1) is described. The convergent synthesis features the use of asymmetric catalysis to generate a chiral cyclopropane fragment and coupling with an indole fragment via an alkyl
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase
Gentles, Robert G.,Ding, Min,Bender, John A.,Bergstrom, Carl P.,Grant-Young, Katharine,Hewawasam, Piyasena,Hudyma, Thomas,Martin, Scott,Nickel, Andrew,Regueiro-Ren, Alicia,Tu, Yong,Yang, Zhong,Yeung, Kap-Sun,Zheng, Xiaofan,Chao, Sam,Sun, Jung-Hui,Beno, Brett R.,Camac, Daniel M.,Chang, Chong-Hwan,Gao, Mian,Morin, Paul E.,Sheriff, Steven,Tredup, Jeff,Wan, John,Witmer, Mark R.,Xie, Dianlin,Hanumegowda, Umesh,Knipe, Jay,Mosure, Kathy,Santone, Kenneth S.,Parker, Dawn D.,Zhuo, Xiaoliang,Lemm, Julie,Liu, Mengping,Pelosi, Lenore,Rigat, Karen,Voss, Stacey,Wang, Yi,Wang, Ying-Kai,Colonno, Richard J.,Gao, Min,Roberts, Susan B.,Gao, Qi,Ng, Alicia,Meanwell, Nicholas A,Kadow, John F.
, p. 1855 - 1879 (2014/04/03)
Described herein are structure-activity relationship studies that resulted in the optimization of the activity of members of a class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors. Subsequent iterations of analogue design and synthe
Compounds for the Treatment of Hepatitis C
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Page/Page column 29, (2009/05/28)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
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Page/Page column 25, (2008/06/13)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
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Page/Page column 43-44, (2008/06/13)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
