1448165-00-1Relevant articles and documents
O2-mediated C(sp2)-X bond oxygenation: Autoxidative carbon-heteroatom bond formation using activated alkenes as a linkage
Lu, Qingquan,Chen, Jiyong,Liu, Chao,Huang, Zhiyuan,Peng, Pan,Wang, Huamin,Lei, Aiwen
, p. 24494 - 24498 (2015)
Autoxidative carbon-heteroatom bond formation using activated alkenes as a linkage is described. Heteroatom (O, S) nucleophiles could be transformed into different kinds of valuable β-keto compounds via an O2-mediated C(sp2)-X bond oxygenation process, without using any external organic oxidants or metal catalysts. This journal is
Synthesis of β-Keto Sulfones by Oxy-Sulfonylation of Alkynes in HFIP
Chen, Xingyu,Lu, Sixian,Zheng, Yuyan,Wang, Jigang,Yang, Lan,Sun, Peng
, p. 1305 - 1312 (2022/03/14)
Herein, we have established a method for the construction of β-keto sulfones through aerobic oxy-sulfonylation of alkynes with sulfinates. The reaction performed employing air as the oxidant and oxygen source. Moreover, this protocol exhibits low consume of sulfinates, short reaction period, and minimal waste. Mechanism study and density functional theory (DFT) calculation showed that the solvent played a significant role in the transformation. (Figure presented.).
Synthesis of β-ketosulfone derivatives as new non-cytotoxic urease inhibitors in vitro
Iqbal Choudhary, M.,Iqbal, Sarosh,Khan, Ajmal,Khan, Khalid Mohammed,Kiran, Shumaila,Nazir, Rashid,Perveen, Shahnaz
, p. 244 - 255 (2020/03/10)
Background: Peptic ulcer and urolithiasis are largely due to infection caused by urease-producing bacteria. Therefore, the discovery of urease inhibitors is an important area of medicinal chemistry research. Objective: The main aim of the work was to identify novel urease inhibitors with no cytotoxicity. Method: During the current study, a series of β-ketosulfones 1-26 was synthesized in two steps and evaluated for their in vitro urease inhibition potential. Results: Out of twenty-six compounds, seventeen have shown good to significant urease inhibitory activity with IC50 values ranging between 49.93-351.46 μM, in comparison to standard thiourea (IC50 = 21 ± 0.11 μM). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line. Conclusion: This study has identified β-ketosulfones as novel and non-cytotoxic urease inhibitors.