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
-
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.
Method for synthesizing azithromycin
-
, (2016/11/17)
The invention relates to a method for synthesizing azithromycin. According to the invention, erythromycin thiocyanate is adopted as an initial raw material of an oximation reaction, such that erythromycin oxime thiocyanate is obtained; the next step of reaction is directly carried out; and through rearrangement, reduction and methylation reactions, azithromycin is obtained. The rearrangement and reduction reactions are carried out with a one-pot method. A reduction reaction product is not separated in a solid form, and is directly used in the methylation reaction. With the synthesizing method provided by the invention, a conversion process from erythromycin oxime thiocyanate to eythromycin oxime is eliminated, and steps that rearrangement and reduction products are separated in solid forms in an original process are also eliminated. The process is environment-friendly and simple, and has the advantages of high yield, low cost, low pollution and high product purity. The method is suitable for industrialized productions.
