107783-01-7Relevant academic research and scientific papers
A Deoxygenative [4+1] Annulation Involving N-Acyldiazenes for an Efficient Synthesis of 2,2,5-Trisubstituted 1,3,4-Oxadiazole Derivatives
Zhou, Rong,Han, Ling,Zhang, Honghui,Liu, Rongfang,Li, Ruifeng
, p. 3977 - 3982 (2017)
An unprecedented and highly efficient tris(dimethylamino)phosphine [P(NMe2)3]-mediated deoxygenative [4 + 1] annulation of N-acyldiazenes with α-dicarbonyl compounds such as isatins, α-keto esters, and α-diketones is reported. The annulation reactions proceed smoothly under mild conditions to deliver a broad range of 2,2,5-trisubstituted 1,3,4-oxadiazole derivatives in moderate to excellent yields from readily available starting materials. It represents the first realization of the [4+1] annulation mode involving N-acyldiazenes to construct five-membered heterocycles. (Figure presented.).
2,2,5-tri-substituted 1,3,4-oxadiazole derivative and synthetic method thereof
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Paragraph 0034; 0035; 0036; 0037; 0038; 0039; 0075-0082, (2018/01/09)
The invention discloses a 2,2,5-tri-substituted 1,3,4-oxadiazole derivative and a synthetic method thereof and belongs to the technical field of organic synthesis. The synthetic method comprises the following steps: reacting N-acyl biazolefin and an alpha-dicarbonyl compound in presence of a three-coordinate phosphrus reagent, thereby obtaining the 2,2,5-tri-substituted 1,3,4-oxadiazole derivative. The synthetic method disclosed by the invention is mild in reaction conditions, wide in substrate application range and high in functional group tolerance; a synthetic technique for efficiently synthesizing the 2,2,5-tri-substituted 1,3,4-oxadiazole derivative with a novel structure is provided; and the invention provides a candidate compound for developing novel oxadiazole pharmaceutical molecules.
