239088-22-3Relevant articles and documents
Synthesis method of special-pulling universal intermediate (by machine translation)
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Paragraph 0024; 0045-0054, (2020/06/20)
To the invention, 9 - 2, 2, 6 tetramethylpiperidine oxide (TEMPO) is used as an oxidizing agent, the reaction temperature 6 - is lower, Fmoc-Cl is protected and oxidized to obtain N - (0 °C fluorenylmethoxycarbonyl) decyl aminoacetaldehyde. TEMPO oxidation is simple, the reaction temperature is mild, pH value and reaction temperature of the reaction liquid are controlled. (by machine translation)
Extra Sugar on Vancomycin: New Analogues for Combating Multidrug-Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococci
Guan, Dongliang,Chen, Feifei,Xiong, Lun,Tang, Feng,Faridoon,Qiu, Yunguang,Zhang, Naixia,Gong, Likun,Li, Jian,Lan, Lefu,Huang, Wei
supporting information, p. 286 - 304 (2018/02/10)
Lipophilic substitution on vancomycin is an effective strategy for the development of novel vancomycin analogues against drug-resistant bacteria by enhancing bacterial cell wall interactions. However, hydrophobic structures usually lead to long elimination half-life and accumulative toxicity; therefore, hydrophilic fragments were also introduced to the lipo-vancomycin to regulate their pharmacokinetic/pharmacodynamic properties. Here, we synthesized a series of new vancomycin analogues carrying various sugar moieties on the seventh-amino acid phenyl ring and lipophilic substitutions on vancosamine with extensive structure-activity relationship analysis. The optimal analogues indicated 128-1024-fold higher activity against methicillin-susceptible S. aureus, vancomycin-intermediate resistant S. aureus (VISA), and vancomycin-resistant Enterococci (VRE) compared with that of vancomycin. In vivo pharmacokinetics studies demonstrated the effective regulation of extra sugar motifs, which shortened the half-life and addressed concerns of accumulative toxicity of lipo-vancomycin. This work presents an effective strategy for lipo-vancomycin derivative design by introducing extra sugars, which leads to better antibiotic-like properties of enhanced efficacy, optimal pharmacokinetics, and lower toxicity.
PROCESS FOR THE PREPARATION OF N-PROTECTED-DECYLAMINOETHANAL
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, (2011/02/24)
Compounds useful in the preparation of telavancin, for example, were prepared. These compounds include decylaminoethanal dialkyl acetals and N-protected decylaminoethanal dialkyl acetals, imidazolidine derivatives, and N-protected- decylaminoethanal.
