239088-22-3Relevant academic research and scientific papers
Synthesis method of special-pulling universal intermediate (by machine translation)
-
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)
VANCOMYCIN DERIVATIVE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
-
, (2019/03/13)
Provided are a class of vancomycin derivatives with a structure as shown in the general formula below and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition containing the compound thereof, and the use of these compounds in preparing drugs for treating and/or preventing bacterial infection diseases, in particular drugs for treating infection diseases caused by Gram-positive bacteria.
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.
Method for preparing telavancin side chain 9H-fluoren-9-ylmethyl decyl(2-oxoethyl)carbamate
-
, (2017/07/01)
The invention discloses a method for preparing telavancin side chain 9H-fluoren-9-ylmethyl decyl(2-oxoethyl)carbamate. The preparation method comprises the following steps: (1) taking n-decanol as an initial raw material, and carrying out oxidation to obtain a n-decanal compound; (2)carrying out reduction amination on the obtained n-decanal compound to obtain N-decyl aminoacetaldehyde dimethyl acetal hydrochloride compound; (3) performing two-step synthesis on N-decyl aminoacetaldehyde dimethyl acetal hydrochloride compound to obtain 9H-fluoren-9-ylmethyl decyl(2-oxoethyl)carbamate compound, wherein the step (3) comprises Fmoc protection and hydrolysis of acetal. The method has the advantages of cheap raw materials, low cost, safe and simple operation, great applicability, being convenient to popularize and apply, and a wide prospect of large-scale industrial application.
PROCESS FOR THE PREPARATION OF N-PROTECTED-DECYLAMINOETHANAL
-
, (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.
Process for preparing glycopeptide derivatives
-
, (2008/06/13)
Disclosed are processes for preparing glycopeptide antibiotic derivatives having an amino-containing side chain. The multi-step process is conducted in a single reaction vessel without isolation of intermediate reaction products.
Process for preparing glycopeptide phosphonate derivatives
-
, (2008/06/13)
Disclosed are processes for preparing glycopeptide phosphonate derivatives having an amino-containing side chain. Several of the process steps are conducted in a single reaction vessel without isolation of intermediate reaction products, thereby generating less waste and improving the overall efficiency and yield of the process.
Process for purifying glycopeptide phosphonate derivatives
-
, (2008/06/13)
Disclosed are methods of purifying glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups that are useful as antibacterial agents. The methods include contacting a solution of the glycopeptide derivatives with a polystyrene-containing resin, eluting the resin with an aqueous solution, and isolating the purified glycopeptide derivative.
Glycopeptide derivatives
-
, (2008/06/13)
Disclosed are derivatives of glycopeptide antibiotic compounds having at least one substituent of the formula: —Ra—Y—Rb—(Z)x where Ra, Rb, Y, Z and x are as defined, and having a group W at the glucose C-6 position, where W is as defined; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Process for perparing N-protected beta-amino aldehyde compounds
-
Page 5, (2008/06/13)
The invention provides processes for preparing N-protected β-amino aldehyde compounds which are useful as synthetic intermediates for preparing glycopeptide antibiotic derivatives. The processes include cleaving a carbon-carbon double bond to form the N-protected β-amino aldehyde compound.
