2417-73-4Relevant articles and documents
REGIOCHEMICALLY CONTROLLED SYNTHESES OF 3-HYDROXYNAPHTO CYCLOBUTENE BY VICINAL DIESTER DIANION CONDENSATION.
Noire, Paul D.,Franck, Richard W.
, p. 1031 - 1034 (1982)
Utilisation of the dianion derived from dimethyl trans-1,2-cyclobutane dicarboxylate allows for the rapid construction of an unsymmetric naphto cyclobutene by two different routes.
Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency
Cushman, Mark,Insaf, Shabana,Paul, Gitendra,Ruell, Jeffrey A.,De Clercq, Erik,Schols, Dominique,Pannecouque, Christophe,Witvrouw, Myriam,Schaeffer, Catherine A.,Turpin, Jim A.,Williamson, Karen,Rice, William G.
, p. 1767 - 1777 (1999)
The anti-HIV agent cosalane inhibits both the binding of gp120 to CD4 as well as an undefined postattachment event prior to reverse transcription. Several cosalane analogues having an extended polyanionic 'pharmacophore' were designed based on a hypothetical model of the binding of cosalane to CD4. The analogues were synthesized, and a number of them displayed anti-HIV activity. One of the new analogues was found to possess enhanced potency as an anti-HIV agent relative to cosalane itself. Although the new analogues inhibited both HIV-1 and HIV-2, they were more potent as inhibitors of HIV-1 than HIV-2. Mechanism of action studies indicated that the most potent of the new analogues inhibited fusion of the viral envelope with the cell membrane at lower concentrations than it inhibited attachment, suggesting inhibition of fusion as the primary mechanism of action.
Design of Chiral NHC-Carboxylates as Potential Ligands for Pd-Catalyzed Enantioselective C?H Activation
Niggli, Nadja E.,Baudoin, Olivier
, (2021/02/26)
Despite numerous efforts, the synthesis of scalemic carbo- and heterocycles through Pd0-catalyzed C(sp3)?H activation employing chiral ancillary ligands or chiral bases is still limited. Inspired by the recently reported outstanding performance of IBiox-type NHC ligands and bifunctional ligands in similar transformations, a new class of bifunctional NHC-ligands bearing a pendant carboxylate group was designed. A library of 10 imidazolium-carboxylic acids was obtained in five to six steps from enantiopure l-tert-leucinol. In addition, four well-defined Pd(DMBPA)-NHC palladacycles were synthesized in good to excellent yields from the corresponding imidazolium precursors. These complexes were tested in a prototypical C(sp3)?H arylation reaction, and the most active one afforded the indoline product in low yield but significant enantioselectivity. These new bifunctional NHCs could find broader applications in catalytic enantioselective transformations occurring under milder conditions.
Polycyclic pyridone derivative, pharmaceutical composition and application thereof
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Paragraph 0127; 0135-0136, (2021/05/01)
The invention belongs to the field of medicines, and relates to a polycyclic pyridone derivative, a pharmaceutical composition and application thereof. The polycyclic pyridone derivative is a compound as shown in a formula (I) or a stereoisomer, a tautomer, a nitric oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the compound as shown in the formula (I). Compared with the existing similar compounds, the compound disclosed by the invention not only can well inhibit the replication of influenza viruses, but also has lower cytotoxicity.
