- Design, synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase
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A number of new F-triazolequinolones (FTQs) and alkoxy-triazolequinolones (ATQs) were designed, synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv. Five out of 21 compounds exhibited interesting minimum inhibitory concen
- Carta, Antonio,Bua, Alessandra,Corona, Paola,Piras, Sandra,Briguglio, Irene,Molicotti, Paola,Zanetti, Stefania,Laurini, Erik,Aulic, Suzana,Fermeglia, Maurizio,Pricl, Sabrina
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p. 399 - 415
(2018/10/31)
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- Acetamidoarenediazonium Salts: Opportunities for Multiple Arene Functionalization
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Unlike their ortho counterparts, meta- and para-acetamidoanilines can be converted into the corresponding acetamidoarenediazonium salts. These offer various opportunities for multiple Pd-catalyzed arene functionalization reactions, such as Matsuda-Heck-, Suzuki-Miyaura- or Fujiwara-Moritani couplings. Acetamidoarenediazonium salts, accessible from simple acetamidoanilines, are starting points for multiple Pd-catalyzed arene functionalization reactions.
- Schmidt, Bernd,Elizarov, Nelli,Riemer, Nastja,H?lter, Frank
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p. 5826 - 5841
(2015/09/15)
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- Elemental fluorine Part 12. Fluorination of 1,4-disubstituted aromatic compounds
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Direct fluorination of a series of 1,4-disubstituted benzene derivatives in acid reaction media at convenient temperature leads, in many cases, to selectively fluorinated aromatic products in preparatively useful conversions and yields.
- Chambers, Richard D.,Hutchinson, John,Sparrowhawk, Matthew E.,Sandford, Graham,Moilliet, John S.,Thomson, Julie
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p. 169 - 173
(2007/10/03)
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- Fluorination process
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According to the present invention there is provided a process for the selective introduction of one or more fluorine atoms into a disubstituted aromatic compound in an acid medium with fluorine gas characterized in that the acid medium has a dielectric constant of at least 20 and a pH of less than 3. The present process provides a cost effective means of selectively introducing one or more fluorine atoms into an aromatic compound in good overall yield.
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- Preparation and alkylation of regioisomeric tetrahydrophthalimide-substituted indolin-2(3H)-ones
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A series of novel regioisomeric tetrahydrophthalimide-substituted indolin-2-ones has been prepared via the Sommelet-Hauser type cyclization of appropriately substituted anilines as potential herbicides. The resultant indolin-2-ones were then regioselectively alkylated at N-1 and C-3 to give 1,3,3-trisubstituted indolin-2-ones. The most active series was also prepared by the bis-nitration of m-fluorophenylacetic acid followed by reduction and cyclization to give 6-amino-5-fluoroindolin-2-one. Elaboration to the tetrahydrophthalimide-substituted indolin-2-one was followed by C- and N-alkylation to give the desired compounds.
- Karp,Condon
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p. 1513 - 1520
(2007/10/02)
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- Synthesis of Asymmetrically Substituted Aminohalogenobenzimidazoles
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2-Fluoroacetanilide (1) upon treatment with HNO3-H2SO4 at -5 to 0 deg C gave 6-fluoro-4-nitroacetanilide (3) whereas at -20 to -10 deg C the product was 6-fluoro-3,4-dinitroacetanilide (5).Although the formation of compound (5) could be accounted for by a conventional nitration mechanism, the fact that (3) could not be nitrated to give (5) and that (5) was formed at a lower temperature than was (3) suggested that the reaction might proceed via an ipso δ intermediate (2).Deacetylation of (5) followed by reduction and condensation with formic acid in the presence of HCl gave 6(5)-fluoro-5(6)-formylaminobenzimidazole (11), 5(6)-amino-6(5)-fluorobenzimidazole (12) and 5-amino-4-chloro-6-fluorobenzimidazole (13).Reduction of (5) with tin followed by condensation with acetic acid gave 5(6)-amino-6(5)-fluoro-2-methylbenzimidazole (14).Concomitant reduction and cyclisation of 6-chloro-2,4-dinitroaniline with formic acid and HCl gave a mixture of 7(4)-chloro-5(6)-formylaminobenzimidazole (15) and 5-amino-4,7-dichlorobenzimidazole (16).
- Camarasa, Maria-Jose,Coe, Paul L.,Jones, A. Stanley,Walker, Richard T.
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p. 2317 - 2320
(2007/10/02)
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