2142-06-5Relevant articles and documents
Iridium-catalyzed double incorporation reaction of N-benzylmaleimide to styrene via ortho-C-H bond activation, initiated by precoordination of the double bond of styrene to iridium
Kiyooka, Syun-Ichi,Takeshita, Yushi
, p. 4279 - 4282 (2005)
Reaction of styrene with N-benzylmaleimide in the presence of [IrCl(cod)]2 (5 mol %) and bpy (10 mol %) in an autoclave (1 MPa of Ar) at 150°C for 18 h stereoselectively led to the formation of a new cyclic product. The structure of the product suggests that a novel iridium-catalyzed double incorporation reaction takes place via a metallacyclopentane formed after ortho-C-H activation.
Photoredox/Cobalt-Catalyzed C(sp3)-H Bond Functionalization toward Phenanthrene Skeletons with Hydrogen Evolution
Guo, Jia-Dong,Yang, Xiu-Long,Chen, Bin,Tung, Chen-Ho,Wu, Li-Zhu
supporting information, p. 9627 - 9632 (2020/12/21)
The first example of photoredox strategy for synthesis of phenanthrene skeletons through C(sp3)-H functionalization under external oxidant-free conditions is achieved. This transformation relies on the keto-enol tautomerism of 1,3 dicarbonyl moiety, i.e., the enol form of 1,3-dicarbonyl derivatives with relatively lower oxidation potential can be activated by the excited acridinium photocatalyst. The electron and proton eliminated from the substrate are immediately captured by a cobaloxime catalyst to exclusively afford a-carbonyl radical for highly substituted 10-phenanthrenols in good to excellent yields.
NOVEL UREA 6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 31, (2020/05/29)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
NOVEL UREA 6,7-DIHYDRO-4H-PYRAZOLO[4,3-C]PYRIDINES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 33, (2020/05/29)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
NOVEL 6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 78, (2020/05/29)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for mating the compounds.
NOVEL INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 120, (2020/11/13)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
NOVEL INDOLIZINE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 91, (2020/11/12)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
NOVEL PHENYL AND PYRIDYL UREAS ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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Page/Page column 112, (2020/11/13)
The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
Preparation method of N-(aryl/heteroaryl) alkyl-diamide
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Paragraph 0052-0053, (2020/12/29)
The invention relates to a preparation method of N-(aryl/heteroaryl)alkyl- diamide, which comprises the following steps: under the protection of nitrogen, sequentially adding transition metal, phosphine or nitrogen ligand, cocatalyst, alkali, solvent, Nhalogenated cyclodiamide, alkyl aromatic ring or alkyl heteroaromatic ring compound into a reaction container, carrying out oxidative amination reaction at 80-140 DEG C, and till the reaction concludes after 6-48 hours, evaporating and drying a solvent and carrying out column chromatography separation to obtain an N (aryl/heteroaryl) alkyl diamide compound. The invention is simple in synthesis process, mild in reaction condition, high in yield and easy to industrialize.
A Unified Strategy for the Synthesis of Difluoromethyl- And Vinylfluoride-Containing Scaffolds
Duchemin, Nicolas,Buccafusca, Roberto,Daumas, Marc,Ferey, Vincent,Arseniyadis, Stellios
supporting information, p. 8205 - 8210 (2019/10/16)
Here, we report a general method for the synthesis of quaternary and tertiary difluoromethylated compounds and their vinylfluoride analogues. The strategy, which relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and either a palladium-catalyzed decarboxylative protonation or a Krapcho decarboxylation, is practical, scalable, and high yielding. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.