123558-64-5Relevant academic research and scientific papers
Atom transfer radical cyclization of trichloroacetamides to electron-rich acceptors using Grubbs' catalysts: Synthesis of the tricyclic framework of FR901483
Diaba, Faza,Martnez-Laporta, Agustn,Bonjoch, Josep
, p. 9365 - 9372 (2014)
Intramolecular Kharasch-type additions of trichloroacetamides on anisole and enol acetates catalyzed by Grubbs' ruthenium carbenes are described. This protocol provides access to highly functionalized 2-azaspiro[4.5]decanes, morphan compounds, and the aza
Synthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage
Zhang, Yuanyuan,Xie, Chuan,Liu, Yang,Shang, Feng,Shao, Rushiya,Yu, Jing,Wu, Chunxia,Yao, Xinghui,Liu, Dongfang,Wang, Zhouyu
, p. 764 - 775 (2021/03/29)
Antibiotics resistance is becoming increasingly common, involving almost all antibiotics on the market. Diseases caused by drug resistant bacteria, such as MRSA, have high mortality and negatively affect public health. The development of new drugs would be an effective means of solving this problem. Modifications based on bioactive natural products could greatly shorten drug development time and improve success rate. Pleuromutilin, a natural product from the basidiomycete bacterial species, is a promising antibiotic candidate. In this study, a series of novel pleuromutilin derivatives possessing piperazinyl urea linkage were efficiently synthesised, and their antibacterial activities and bactericidal properties were evaluated via MIC, MBC and Time-kill kinetics assays. The results showed that all compounds exhibited potent activities against tested strains, especially MRSA strains with MIC values as low as 0.125 μg/mL; 8 times lower than that of marketed antibiotic Tiamulin. Docking studies indicate substituted piperazinyl urea derivatives could provide hydrogen bonds and initiate π-π stacking between molecules and surrounding residues.
Rearrangement of Benzylic Trichloroacetimidates to Benzylic Trichloroacetamides
Adhikari, Arijit A.,Suzuki, Tamie,Gilbert, Reesheda T.,Linaburg, Matthew R.,Chisholm, John D.
, p. 3982 - 3989 (2017/04/11)
The rearrangement of allylic trichloroacetimidates is a well-known transformation, but the corresponding rearrangement of benzylic trichloroacetimidates has not been explored as a method for the synthesis of benzylic amines. Conditions that provide the tr
NEW PROCEDURES FOR THE SYNTHESIS OF SYMMETRICAL BISBENZYLATED UREAS BASED ON N-BENZYLTRICHLOROACETAMIDES
Atanassova, I.A.,Petrov, J.S.,Mollov, N.M.
, p. 147 - 154 (2007/10/02)
Treatment of N-benzylated trichloroacetamides 4, obtained by three different procedures, with potassium carbonate in dimethylsulfoxide affords simmetrical bisbenzylated ureas 5.
