- Palladium-Catalyzed β-Arylation of Amide via Primary sp3C-H Activation
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A β-arylation of primary sp3C-H bonds on simple amides such as pivalamides with aryl iodides/CF3CO2Ag has been established successfully at 120 °C in a Pd(OAc)2 (catalyst)/CF3CH2OH (solvent) system. Pivalamides including tBuCONH2, tBuCONHR, and tBuCONR2 undergo the arylations smoothly to afford β-aryl pivalamides in moderate to good yields. Various aryl iodides are available bearing either electron-donating or electron-withdrawing substituted groups in the coupling reactions.
- Zhao, Ren,Lu, Wenjun
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supporting information
p. 2188 - 2192
(2018/07/25)
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- QUINAZOLINONE DERIVATIVES AS VIRAL POLYMERASE INHIBITORS
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Compounds of formula I: (I) wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
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Page/Page column 49
(2011/04/19)
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- BIS-AROMATIC COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATION
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There is provided compounds of formula (I): wherein Y, ring A, D1, D2, D3, L1, Y1, L2, Y2, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
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Page/Page column 28
(2010/12/29)
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- BIS AROMATIC COMPOUNDS FOR USE AS LTC4 SYNTHASE INHIBITORS
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There is provided compounds of formula (I), wherein E1, E2a, E2b, E2c, E4, D1, D2, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
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Page/Page column 64
(2010/10/03)
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- VIRAL POLYMERASE INHIBITORS
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Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
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Page/Page column 68
(2009/04/25)
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- VIRAL POLYMERASE INHIBITORS
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Compounds of formula I: wherein X, R2, R3, R3a, R3b,R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
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Page/Page column 61
(2009/07/18)
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
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Page/Page column 39
(2010/11/28)
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- BENZOXAZINYL-AMIDOCYCLOPENTYL-HETEROCYCLIC MODULATORS OF CHEMOKINE RECEPTORS
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Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula (I): which are used to modulate the CCR-
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