- Chemoselective acylation of benzimidazoles with phenylacetic acids under different Cu catalysts to give fused five-membered N-heterocycles or tertiary amides
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C-N bond formation via a copper-catalyzed aerobic oxidative decarboxylative tandem protocol was realized. The phenylacetic acids which contain ortho-X (X = F or Br) on the aromatic ring will render a fused five-membered heterocycle via a tandem aromatic nucleophilic substitution and aerobic oxidative decarboxylative acylation at the C(sp2)-H bond of benzimidazoles under the Cu(OAc)2/K2CO3/BF3·Et2O catalytic system, while with CuBr as the catalyst and pyridine as the base, N-acylation occurred and tertiary amides were obtained.
- Mai, Shaoyu,Zhao, Yingwei,Song, Qiuling
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supporting information
p. 8685 - 8690
(2016/10/03)
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- Iron-catalyzed synthesis of polycyclic-fused azo[l,2-a]indolones via an SNAr/acylation cascade reactions
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An efficient method has been developed for the cascade synthesis of azo[l,2-a]indolones from azoles and 2-fluoroaldehydes based on an iron-catalyzed SNAr and a direct acylation reaction. A number of azo[l,2-a]indolones containing different azol
- Yang, Jian-Guo,Xu, Ling-Zhen,Huang, Ling,Gao, Jian-Rong,Liu, Miao-Chang,Pan, Fu-You,Chen, Ding-Ben
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p. 340 - 344
(2016/03/16)
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- A triazolo indol the alkone is thick heterocyclic high efficient synthesis method
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The invention relates to an efficient synthesis method for 11 hydrogen-indole [1, 2-a] benzimidazole-11-ketone, 9 hydrogen-imidazole [1, 2-a] indole-9-ketone and 11 hydrogen-indole [1, 2-a] indazole-11-ketone. The method comprises the following steps: using ferric salt as a catalyst, and in the existence of air, using substituted 2-fluorobenzaldehyde and three types of different azole heterocycles as raw materials to have the one-pot reaction of SN2 nucleophilic substitution/carbon-hydrogen activation/acylation and cyclization to synthesize corresponding products. The synthesis method disclosed by the invention is simple and convenient, the raw materials are easy to obtain, and the method is efficient and novel. The method can provide a novel synthesis route for drug molecules or bioactivity substances containing the three types of condensed heterocycles.
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Paragraph 0048-0051
(2016/12/01)
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- Synthesis of polycyclic indolone and pyrroloindolone heterocycles via the annulation of indole- and pyrrole-2-carboxylate esters with arynes
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A mild and general method for the synthesis of a variety of polycyclic indolone and pyrroloindolone heterocycles via the reaction of indole- and pyrrole-2-carboxylate esters with arynes has been developed. Georg Thieme Verlag Stuttgart.
- Giacometti, Robert D.,Ramtohul, Yeeman K.
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scheme or table
p. 2010 - 2016
(2010/04/04)
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- Cyclization Reactions in Azole Chemistry: The Reaction of Some Azoles with o-Fluoroacetophenone, o-Fluorobenzaldehyde and o-Fluorobenzophenone
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The reactions of some azoles with o-fluoro-acetophenone, -benzaldehyde and -benzophenone in dimethyl sulfoxide solution in the presence of anhydrous potassium carbonate have been investigated.In addition to the expected substitution products, cyclization
- Rosevear, Judi,Wilshire, John F. K.
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p. 1097 - 1114
(2007/10/02)
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