20430-72-2Relevant articles and documents
Sulfone-Mediated SNAr Reaction as a Powerful Tool for the Synthesis of 4-Quinolinyl Ethers and More-Application to the Synthesis of HCV NS3/4a Protease Inhibitor BI 201420
Patel, Nitinchandra D.,Wei, Xudong,Byrne, Denis,Narayanan, Bikshandarkoil A.,Pennino, Scott,Sarvestani, Max,Saha, Anjan,Haddad, Nizar,Kapadia, Suresh,Lorenz, Jon C.,Decroos, Philomen,Ye, Andrew,Lee, Heewon,Grinberg, Nelu,Hossain, Azad,Busacca, Carl A.,Yee, Nathan K.,Senanayake, Chris H.
, p. 8339 - 8351 (2020/07/16)
An efficient general methodology for the synthesis of 4-quinolinyl ethers is demonstrated via a highly reactive SNAr reaction of 4-quinolinyl sulfones with a range of structurally diversified 1°, 2°, and 3° alcohols with a wide substrate scope and high yields. By adapting this methodology, a convergent synthesis of a complex target of HCV NS3/4a protease inhibitor BI 201420 was accomplished.
2-aryl-4-quinolone derivative as well as preparation method and application thereof
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Paragraph 0054-0060, (2018/10/19)
The invention discloses a 2-aryl-4-quinolone derivative as well as a preparation method and an application thereof. The 2-aryl-4-quinolone derivative has the structure shown in formula (I) in the description, wherein R1 is independently selected from one or more of H, C1-C5 alkyl, halogen or C1-C5 alkoxy, and R2 is independently selected from one or more of H, C1-C5 alkyl, CF3, halogen or C1-C5 alkoxy. Test results show that the 2-aryl-4-quinolone derivative has good antibacterial activity and can be used as an antibacterial agent.
Microwave-assisted synthesis of polysubstituted 4-quinolones from deprotonated α-aminonitriles
Romek, Alexandra,Opatz, Till
experimental part, p. 5841 - 5849 (2011/01/04)
The α-alkylation of deprotonated N-aryl-α-aminonitriles with α-bromoesters furnishes intermediates that can be cyclized to 4-quinolones upon microwave irradiation. Alternatively, base-induced dehydrocyanation of the alkylation products furnishes enaminoes
Hepatitis C Virus Inhibitors
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Page/Page column 27-28, (2009/12/02)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Macrocyclic Inhibitors of Hepatitis C Virus
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Page/Page column 43, (2009/02/11)
Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR1, NHS(═O)pR2, NHR3, NRaRb, C(═O)NHR3 or C(═O)NRaRb wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl or NRaRb; R3 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, —OC1-C6alkyl, —OC0-C3alkylenecarbocyclyl, —OC0-C3alkyleneheterocyclyl; wherein any alkyl, carbocyclyl or heterocycylyl in R1, R2 or R3 are optionally substituted p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Ry and Ry′ are independently C1-C6alkyl; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; W is —CH2—, —O—, —OC(═O)NH—, —OC(═O)—, —S—, —NH—, —NRa, —NHS(═O)2—, —NHC(=0)NH— or —NHC(═O)—, —NHC(═S)NH— or a bond; R8 is an optionally substituted ring system containing 1 or 2 saturated, partially saturated or unsaturated carbo or heterocyclic rings have utility in the inhibition of NS-3 serine proteases, such as flavivirus infections.
NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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, (2009/10/31)
The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
A mild, one-pot synthesis of 4-quinolones via sequential Pd-catalyzed amidation and base-promoted cyclization
Huang, Jinkun,Chen, Ying,King, Anthony O.,Dilmeghani, Mina,Larsen, Robert D.,Faul, Margaret M.
supporting information; experimental part, p. 2609 - 2612 (2009/05/27)
(Chemical Equation Presented) A mild, one-pot synthesis of 4-quinolones is described. Under the optimal conditions, a variety of 2-substituted 4-quinolones were synthesized via sequential palladium-catalyzed amidation of 2′-bromoacetophenones followed by base-promoted intramolecular cyclization.
HCV NS-3 serine protease inhibitors
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, (2008/06/13)
HCV inhibitors, compositions comprising these compounds as active ingredient, as well as processes for preparing these compounds, having the formula I wherein A is
HCV NS-3 serine protease inhibitors
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, (2008/06/13)
HCV inhibitors, compositions comprising these compounds as active ingredient, as well as processes for preparing these compounds, of formula: wherein A is
Hepatitis C virus inhibitors
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Page/Page column 33-34, (2008/06/13)
The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which inhibit the function of the NS3 protease (also referred to herein as “serine protease”) encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS3 protease.
