342371-84-0Relevant articles and documents
Synthesis and antibacterial activity of new 4″-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether
Zhang, Ling,Jiao, Bo,Yang, Xiangrui,Liu, Lin,Ma, Shutao
, p. 243 - 247 (2011)
A series of new 4″-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether were synthesized and evaluated for their in vitro antibacterial activity. All the desired compounds demonstrated favorable activity (0.03 μg ml-1) against erythromycin-susceptible Streptococcus pneumoniae comparable to the references, exhibiting 133-fold higher activity than precursor 2 or 3. Similarly, all of the analogs exhibited improved activity against the erythromycin-resistant S. pneumoniae encoded by the erm gene and the erm and mef genes, showing 4-32-fold more effectiveness than erythromycin A.
Synthesis method of azithromycin
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Paragraph 0003; 0025-0026, (2017/08/29)
The invention relates to a synthesis method of azithromycin. The synthesis method is characterized by comprising the process steps of firstly adding sodium bicarbonate and a rearrangement reaction reagent to erythromycin oxime in a reaction system employing water as a reaction solvent for rearrangement reaction, carrying out heat preservation for 2-3 hours, dropwise adding a reduction reaction regent for reduction reaction and stirring for 1-2 hours during heat preservation; adding a competitive inhibitor for removing boron through reduction hydrolysis for reduction and boron removal reaction; and finally separating out crystal, and cooling and filtering to obtain the azithromycin. Rearrangement and reduction are simultaneously carried out in the same reaction system. Compared with a sodium borohydride reduction method in the prior art, the synthesis method has the advantages that the process is simplified, use of an organic solvent and the like is omitted, the environmental pollution and the product cost are reduced, the influence of a complicated process on the quality of a product is reduced, the quality and the yield of the product are finally improved and the synthesis method is suitable for technological production.
Preparation method of erythromycin 6,9-imino ether compound
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Paragraph 0021, (2017/04/25)
The invention relates to a preparation method of an erythromycin 6,9-imino ether compound. According to the method, a reaction of acid-catalyzed erythromycin thiocyanate and N-hydroxyamide is adopted, an oximation reaction of erythromycin and a rearrangement reaction of erythromycin oxime are conducted in a one-step mode, and erythromycin 6,9-imino ether is generated. The preparation method of the compound comprises the preparation steps that erythromycin thiocyanate, N-hydroxyamide and acid are taken and added into an organic solvent, heating is conducted, extracting, drying by distillation and water adding are conducted after the reaction is completed, the pH value of the solution is adjusted to range from 10 to 12, precipitating, filtering and drying are conducted, and the erythromycin 6,9-imino ether product is obtained. According to the preparation method, the erythromycin 6,9-imino ether compound is synthesized in a one-step mode, operation is easy, the method is economical and efficient, a venomous sulfonyl chloride reagent is not used, environmental pollution is less, the yield is high, and the application prospect is wide.
