- Synthesis of 2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinolin-4-ol; A quinoline building block for simeprevir synthesis
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Two synthetic approaches to the achiral quinoline fragment of simeprevir are described. Both approaches are based on the synthesis of methyl 4-hydroxy-7-methoxy-8-methylquinoline-2-carboxylate, protection of its 4-hydroxyl group, and construction of the thiazole ring from the ester group at the 2-position. The last step is acid deprotection of the 4-hydroxyl protecting group. Georg Thieme Verlag Stuttgart. New York.
- Rádl, Stanislav,Rezková, Hana,Obadalová, Iva,Srbek, Jan,B?ichá?, Ji?í,Pekárek, Tomá?
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p. 899 - 908
(2014/04/03)
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- Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335)
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C-Terminal carboxylic acid containing inhibitors of the NS3 protease are reported. A novel series of linear tripeptide inhibitors that are very potent and selective against the NS3 protease are described. A substantial contribution to the potency of these
- Llinàs-Brunet, Montse,Bailey, Murray D.,Goudreau, Nathalie,Bhardwaj, Punit K.,Bordeleau, Josée,B?s, Michael,Bousquet, Yves,Cordingley, Michael G.,Duan, Jiamin,Forgione, Pat,Garneau, Michel,Ghiro, Elise,Gorys, Vida,Goulet, Sylvie,Halmos, Ted,Kawai, Stephen H.,Naud, Julie,Poupart, Marc-André,White, Peter W.
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experimental part
p. 6466 - 6476
(2010/11/04)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
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