- The Direct C-4 Substitution of Indole; An X-Ray Crystal Structure Analysis of 4-(Trimethylsilyl)indole
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Indole was converted into the 1,4-diacetyl and 1-acetyl-4-(3-chloropropanoyl) derivatives by direct C-4 electrophilic substitution via 4-(trimethylsilyl)indole (3c); the structure of (3c) was confirmed by a single crystal X-ray analysis.
- Barrett, Anthony G. M.,Dauzonne, Daniel,Williams, David J.
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- Multinuclear NMR study of compounds resulting from the silylation of indole; evidence for a 4,5-disilylation
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Complete assignments of the 1H, 13C and 29Si NMR data of 1-, 4- and 5-trimethylsilyl-, 1,4- and 1,5-bis(trimethylsilyl)- and 1,4,5-tris(trimethylsilyl)-indoles allowed unambiguous confirmation of the structures proposed for these products.For the trisilylated derivative it was found that silylation had occurred at the 1,4,5 and not at 1,4,7 positions as previously suggested.
- Biran, Claude,Fourtinon, Michel,Efendene, Blaise,Dunogues, Jacques
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- 6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to antiviral agents. Specifically, the present invention relates to compounds of formula I 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.
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Page/Page column 70
(2020/05/29)
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- NOVEL 6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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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.
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Page/Page column 72
(2020/05/29)
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- NOVEL OXALYL PIPERAZINES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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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.
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Page/Page column 87-88
(2020/11/12)
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- NOVEL INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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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.
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- NOVEL, HIGHLY ACTIVE PYRAZOLO-PIPERIDINE SUBSTITUTED INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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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.
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Page/Page column 94
(2019/05/22)
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- NOVEL, HIGHLY ACTIVE AMINO-THIAZOLE SUBSTITUTED INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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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.
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Page/Page column 122
(2019/05/22)
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- Preparation and Reactions of 4-(Trimethylsilyl)indole
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Indole or 1-(trimethylsilyl)indole was reacted sequentially with lithium-chlorotrimethylsilane and with 1,4-benzoquinone to produce 1,4-bis(trimethylsilyl)indole (50 percent and 55 percent, respectively).Methanolysis gave 4-(trimethylsilyl)indole which reacted with electrophiles at C-3.However, the derivative 1-acetyl-4-(trimethylsilyl)indole reacted with acetyl, 2-chloropropanoyl, or propenoyl chlorides via clean C-4 ipso substitution.Attemps to extend the reaction to a useful synthesis of derivatives of 5-oxo-1,3,4,5-tetrahydrobenzindole, a lysergic acid synthon, were prevented by low yields.
- Barrett, Anthony G. M.,Dauzonne, Daniel,O'Neil, Ian A.,Renaud, Alain
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p. 4409 - 4415
(2007/10/02)
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- A New Synthesis of 4-Substituted Indoles via Tricarbonylarenechromium(0) Complexes
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Tricarbonyl-(η6-1-tri-isopropylsilylindole)chromium(0), lithiated selectively at C-4 by n-butyl-lithium-N,N,N',N'-tetramethylethylenediamine (TMEDA), can be substituted in good yield by a range of electrophiles; the method has been used to synthesise 4-prenylindole.
- Nechvatal, Gordon,Widdowson, David A.
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p. 467 - 468
(2007/10/02)
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