- Synthesis method of 3, 5-disubstituted 1, 2, 4-oxadiazole
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The invention relates to a novel synthetic method for synthesizing 3, 5-disubstituted-1, 2, 4-oxadiazole, in particular to a synthetic method of 3, 5-disubstituted-1, 2, 4-oxadiazole. The method disclosed by the invention has the characteristics that the reaction is carried out at room temperature, the 1, 2, 4-oxadiazole is synthesized at high yield by a one-pot method, and a final product does not need to be subjected to column chromatography. The 3, 5-disubstituted-1, 2, 4-oxadiazole synthesized by the invention can be used in the field of medical treatment.
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Paragraph 0027-0030
(2021/06/22)
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- Enol Ester Intermediate Induced Metal-Free Oxidative Coupling of Carboxylic Acids and Arylboronic Acids
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A facile, efficient and environmentally friendly methodology for the preparation of phenolic esters is realized via metal-free coupling of carboxylic acids and arylboronic acids. This sequential one pot reaction, employing methyl propiolate as an activating reagent, proceeds through the formation of enol ester intermediate, followed by a nucleophilic attack on the C-O bond under the oxidation of hydrogen peroxide. These studies display that enol esters, despite previously being overlooked as synthetic intermediates, would be the valuable building blocks for developing carbon–carbon and carbon–heteroatom bond-forming reactions.
- Xu, Xianjun,Feng, Huangdi,Li, Huiqiong,Huang, Liliang
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p. 3921 - 3928
(2019/06/24)
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- Direct Amidation of Carboxylic Acids through an Active α-Acyl Enol Ester Intermediate
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The development of a highly efficient and simple protocol for the direct amidation of carboxylic acids is described employing ynoates as novel coupling reagents. The transformation proceeds in good to excellent yields via in situ α-acyl enol ester intermediates formation under mild reaction conditions. This useful method has been demonstrated for a range of substrates to provide a succinct access to structurally diverse amides, including key intermediates of glibenclamide, tiapride hydrochloride, and nateglinide, and can be conducted on a mole scale.
- Xu, Xianjun,Feng, Huangdi,Huang, Liliang,Liu, Xiaohui
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p. 7962 - 7969
(2018/06/18)
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