90-31-3Relevant articles and documents
Electrochemical synthesis of versatile ammonium oxides under metal catalyst-, exogenous-oxidant-, and exogenous-electrolyte-free conditions
Yuan, Yong,Li, Liang-Sen,Zhang, Lin,Wang, Feng,Jiang, Lin,Zuo, Lin,Wang, Qi,Hu, Jian-Guo,Lei, Aiwen
supporting information, p. 2768 - 2771 (2021/03/23)
An electrochemical oxidative cross-coupling reaction between 2.5-substituted-pyrazolin-5-ones and ammonium thiocyanate has been developed, which resulted in a series of unprecedented cross-coupling products under metal catalyst-, exogenous-oxidant-, and exogenous-electrolyte-free conditions. It is worth noting that since the resulting cross-coupling products are nearly insoluble in MeCN, the pure product could be afforded without silica gel column purification. In addition, the prepared ammonium oxides are versatile building blocks for synthesizing functionalized pyrazole derivatives.
Stereoselective Assembly of Multifunctional Spirocyclohexene Pyrazolones That Induce Autophagy-Dependent Apoptosis in Colorectal Cancer Cells
Li, Xiang,Chen, Fei-Yu,Kang, Jing-Wen,Zhou, Jin,Peng, Cheng,Huang, Wei,Zhou, Mu-Ke,He, Gu,Han, Bo
, p. 9138 - 9150 (2019/08/12)
Enantio- and diastereoselective synthesis of multifunctional spiropyrazolone scaffolds has been achieved using secondary amine-catalyzed [4 + 2] annulations of α,β,γ,δ-unsaturated pyrazolones with aldehydes. The pyrazolone substrates serve as C4 synthons to produce 6-membered, carbocycle-based, chiral spiropyrazolone derivatives. The synthesized chiral compounds showed potent toxicity against a panel of cancer cell lines. The most potent compound 3h-induced cell cycle arrest and macroautophagy in HCT116 colorectal cancer cells, triggering autophagy-dependent apoptotic cell death.
Pyrazolone and synthetic method of derivative of pyrazolone
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Paragraph 0060; 0061, (2018/03/26)
The invention relates to pyrazolone and a synthetic method of a derivative of pyrazolone. The method comprises the steps of preparing acetylacetamide with ketene dimer and ammonium hydroxide being rawmaterials in an ammoniation phase; directly adding substituted hydrazine into an ammoniation kettle to be subjected to a condensation reaction in a condensation phase; adopting concentrated hydrochloric acid to adjust the PH to promote proceeding of a ring-closure reaction in a ring-closure phase; using a cleaning solvent to conduct cleaning to obtain a purified product during aftertreatment. According to the synthetic method, a one-pot method is utilized to synthesize a pyrazolone compound free of solvents, since no solvents exist, the separation and purification process of the product are easily carried out, green production of fine chemicals is effectively achieved, the operation is convenient, the reaction time is obviously shortened, high yield of the product with excellent appearance is achieved, the product yield is increased, the product quality is improved, the yield can reach 88%-98%, and the purity can reach 96%-98%; meanwhile, drainage of wastewater is greatly reduced, andthe problems that the environment pollution is caused, the health of the human kind is harmed, and resources are wasted when water serves as a solvent are fundamentally solved.