90534-46-6Relevant articles and documents
AMINOALKYL PHENOL ETHER INHIBITORS OF INFLUENZA A VIRUS
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Page/Page column 34, (2013/06/05)
The present invention is directed to the discovery of novel nonpeptidic small molecules that function as inhibitors of the influenza virus infection. In particular, the present invention is directed to the discovery of anti-influenza entry inhibitors with
QSAR study for?a?novel series of?ortho disubstituted phenoxy analogues of?α1-adrenoceptor antagonist WB4101
Pallavicini,Fumagalli,Gobbi,Bolchi,Colleoni,Moroni,Pedretti,Rusconi,Vistoli,Valoti
, p. 1025 - 1040 (2007/10/03)
On the basis of the affinities at the α1a-, α1b- and α1d-adrenoceptors and the 5-HT1A receptor of a previous series of sixteen 2-[(2-phenoxyethyl)aminomethyl]-1,4-benzodioxanes ortho monosubstituted at the pheno
Development of a scalable process for CI-1034, an endothelin antagonist
Jacks, Thomas E.,Belmont, Daniel T.,Briggs, Christopher A.,Horne, Nicole M.,Kanter, Gerald D.,Karrick, Greg L.,Krikke, James J.,McCabe, Richard J.,Mustakis, Jason G.,Nanninga, Thomas N.,Risedorph, Guy S.,Seamans, Ronald E.,Skeean, Richard,Winkle, Derick D.,Zennie, Thomas M.
, p. 201 - 212 (2013/09/04)
A concise, convergent multikilogram synthesis of CI-1034 (1), a potent endothelin receptor antagonist, is described. A 15-step preparation from commercially available o-vanillin and benzenesulfonyl chloride employs a remarkably robust Suzuki coupling between a boronic acid and an aromatic sulfonate ester as the key synthetic step. A scalable route capable of producing multikilogram quantities of CI-1034 with no chromatographic steps is described in this contribution. Improvements to the process included using a 4-fluorobenzenesulfonate ester as a suitable substitute for the triflate group in the Suzuki reaction and the use of MgCl2 as a substitute for TiCl4 in a Dieckmann condensation to provide the benzothiazine dioxide core.
Isolation, Synthesis, Structure-Activity Relationships of Bioactive Benzoquinones from Miconia lepidota from the Suriname Rainforest
Gunatilaka, A. A. Leslie,Berger, John M.,Evans, Randy,Miller, James S.,Wisse, Jan H.,Neddermann, Kim M.,Bursuker, Isia,Kingston, David G. I.
, p. 2 - 5 (2007/10/03)
Bioactivity-directed fractionation of an EtOAc extract from the leaves of Miconia lepidota afforded the two benzoquinones 2-methoxy-6-heptyl-1,4-benzoquinone (1) and 2-methoxy-6-pentyl-1,4-benzoquinone (primin) (2). This is the first reported isolation of
Synthesis of Side-Chain-Modified Analogues of the Allergen Primin
Koenig, Wilfried A.,Faasch, Holger,Heitsch, Holger,Colberg, Cornelia,Hausen, Bjoern M.
, p. 387 - 393 (2007/10/02)
Benzoquinones such as primin (2-methoxy-6-pentyl-1,4-benzoquinone) from Primula obconica HANCE (Primulaceae) are known to be strong sensitizers and thus the source of severe allergic contact dermatitis (cell-mediated type of allergy).In order to determine
Tobacco smoke chemistry. 2. Alkyl and alkenyl substituted guaiacols found in cigarette smoke condensate.
Arnarp,Bielawski,Dahlin,Dahlman,Enzell,Pettersson
, p. 44 - 50 (2007/10/02)
A series of alkyl and alkenyl substituted guaiacols, which comprise a group of biologically and organoleptically active compounds, have been synthesized. Mass spectra and GC retention times for these have been recorded and compared with those obtained for constituents of a weakly acidic fraction of smoke condensate derived from American blend type cigarettes. On the basis of these results, 25 guaiacols have been identified, 18 of which have not been detected in tobacco smoke condensate previously.