13114-70-0Relevant academic research and scientific papers
Synthesis method of substituted urea compound
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Paragraph 0034-0039; 0114-0119, (2021/03/31)
The invention discloses a synthesis method of a substituted urea compound, which comprises the following steps: stirring aldehyde, N-aryl urea, trichlorosilane and Lewis base in an organic solvent ata temperature range of -20 DEG C to room temperature for
Photocatalyzed synthesis of unsymmetrical ureas via the oxidative decarboxylation of oxamic acids with PANI-g-C3N4-TiO2 composite under visible light
Wang, Liang,Wang, Hao,Wang, Yaoyao,Shen, Minggui,Li, Shubai
supporting information, (2020/04/28)
The synthesis of unsymmetrical ureas via the photocatalyzed oxidative decarboxylation of oxamic acids has been developed. The carbamoyl radicals were generated from oxamic acids in the presence of a hypervalent iodine reagent and the PANI(Polyaniline)-g-C3N4-TiO2 composite under visible light irradiation. The radicals were converted in situ into the corresponding isocyanates, which were then trapped by amines to afford the corresponding products in moderate to good yields. This protocol avoided the direct use of environmentally unfriendly isocyanates and a series of substrates were tolerated. Moreover, the photocatalyst could be readily recovered by simple filtration and be reused for several runs with only a slight decrease in the catalytic activity.
Biochemical and microbiological evaluation of: N-aryl urea derivatives against mycobacteria and mycobacterial hydrolases
Vartak, Abhishek,Goins, Christopher,De Moura, Vinicius Calado Nogueira,Schreidah, Celine M.,Landgraf, Alexander D.,Lin, Boren,Du, Jianyang,Jackson, Mary,Ronning, Donald R.,Sucheck, Steven J.
, p. 1197 - 1204 (2019/07/25)
A focused library of 24 N-aryl urea derivatives was prepared and evaluated against serine esterases of Mycobacterium tuberculosis (Mtb) Rv3802c and Mtb Ag85C. The members of the library were evaluated for both selectivity and mode of inhibition. Furan-bas
Pd/C-Catalyzed Domino Synthesis of Urea Derivatives Using Chloroform as the Carbon Monoxide Source in Water
Wang, Liang,Wang, Hao,Li, Guiqing,Min, Shuliang,Xiang, Fangyuan,Liu, Shiqi,Zheng, Waigang
, p. 4585 - 4593 (2018/10/31)
A Pd/C-catalyzed domino synthesis of symmetrical and unsymmetrical ureas from aryl iodides, sodium azide, amines and CHCl3 in water has been developed. This reaction proceeds with sequential carbonylation, Curtius rearrangement and nucleophilic addition. CHCl3 serves as a convenient and safe alternation of CO gas in the presence of KOH. A series of urea derivatives were obtained in moderate to good yields with good functional group tolerance. Furthermore, the Pd/C catalyst could be readily recovered with slight decrease in the catalytic activity after six consecutive runs. (Figure presented.).
Degradable conjugates from oxanorbornadiene reagents
Kislukhin, Alexander A.,Higginson, Cody J.,Hong, Vu P.,Finn
supporting information; experimental part, p. 6491 - 6497 (2012/05/07)
Oxanorbornadienedicarboxylate (OND) reagents were explored for purposes of binding and releasing drugs from serum albumins as representative macromolecular carriers. Being highly reactive Michael acceptors, ONDs form adducts with thiols and amines, which then undergo retro-Diels-Alder fragmentation. A study of more than 30 model adducts revealed a number of modifications that can be used to influence adduct stability. For the most reactive OND linkers, the labeling of the single available bovine serum albumin (BSA) cysteine residue was complete within minutes at a mid-micromolar concentration of reactants. While a selectivity of greater than 1000-fold for thiol over amine was observed with model amino acids, the labeling of protein amines with ONDs is fast enough to be practical, as demonstrated by the reaction with thiol-depleted BSA. The OND-amine adducts were found to be up to 15 times more stable than OND-thiol adducts, and to be sensitive to acid by virtue of a stereochemically dependent acceleration of cycloreversion. The release rate of fluorescent cargo from serum albumins was tuned by selecting the coupling partners: the available half-lives ranged from 40 min to 7 days at 37 °C. Such versatility of release profiles from protein carriers, controlled by the nature of the OND linkage, is a useful addition to the drug delivery toolbox.
