59681-66-2Relevant articles and documents
Cu-Catalyzed C-H Allylation of Benzimidazoles with Allenes
Dong, Yaxi,Breit, Bernhard
supporting information, p. 6765 - 6769 (2021/09/11)
CuH-catalyzed intramolecular cyclization and intermolecular allylation of benzimidazoles with allenes have been described. The reaction proceeded smoothly with the catalytic system of Cu(OAc)2/Xantphos and catalytic amount of (MeO)2MeSiH. This protocol features mild reaction conditions and a good tolerance of substrates bearing electron-withdrawing, electron-donating, or electron-neutral groups. A new catalytic mechanism was proposed for this copper hydride catalytic system.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000315, (2015/04/15)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly
Fader, Lee D.,Bethell, Richard,Bonneau, Pierre,B?s, Michael,Bousquet, Yves,Cordingley, Michael G.,Coulombe, René,Deroy, Patrick,Faucher, Anne-Marie,Gagnon, Alexandre,Goudreau, Nathalie,Grand-Ma?tre, Chantal,Guse, Ingrid,Hucke, Oliver,Kawai, Stephen H.,Lacoste, Jean-Eric,Landry, Serge,Lemke, Christopher T.,Malenfant, Eric,Mason, Stephen,Morin, Sébastien,O'Meara, Jeff,Simoneau, Bruno,Titolo, Steve,Yoakim, Christiane
scheme or table, p. 398 - 404 (2011/03/17)
The discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly is described. Synthesis of analogs of the 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione hit established structure-activity relationships. Replacement of the enamine functionality of the hit series with either an imidazole or a pyrazole ring led to compounds that inhibited both capsid assembly and reverse transcriptase. Optimization of the bicyclic benzodiazepine scaffold to include a 3-phenyl substituent led to lead compound 48, a pure capsid assembly inhibitor with improved antiviral activity.