13127-18-9Relevant articles and documents
Translactonization of erythromycin a during oximation: Mixture analysis and reaction monitoring by NMR
Grover, Rajesh K.,Joshi,Batra,Roy, Raja,Bhaduri
, p. 355 - 360 (2001)
Oximation of erythromycin A with hydroxylamine hydrochloride and sodium acetate in methanol led to the formation of pseudoerythromycin A enol ether with erythromycin A oxime as analysed by detailed two-dimensional NMR spectroscopy in the mixture along with traces of 8,9-anhydroerythromycin A 6,9-hemiketal and erythromycin A 6,9:9,12-spiroketal. The formation of the degraded products was established by performing in situ 13C NMR spectroscopy. The analysis suggests that pseudoerythromycin A enol ether is formed by the translactonization of erythromycin A enol ether which forms as a result of acid degradation. Copyright
Synthesis of two and antibacterial activity of one novel oxime ether derivatives of erythromycin A
Dondas,Yaktubay
, p. 1011 - 1015 (2003)
The synthesis of novel erythromycin A 9-O-(2-ethenesulfony-ethyl)-oxime and erythromycin A 9-O-(3-oxo-butyl)-oxime from erythromycin A (EA) by the Michael reaction is described and to describe the effects of transformation of ketone in position 9 of EA to an oxime ether. This transformation occurred in a single step without protecting of any functional moiety of erythromycin oxime and zero waste manner in good yield. The antibacterial screen of EA 9-O-(2-ethenesulfony-ethyl)-oxime is also reported.
Synthetic method of isotope-labeled erythromycylamine
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Paragraph 0020; 0025-0027; 0033-0035; 0041-0043, (2020/07/28)
The invention discloses a synthetic method of isotope-labeled erythromycylamine, belongs to the field of drug metabolism, and provides a synthetic method which is reasonable in process design, strongin operability and high in yield, can efficiently convert isotope-labeled raw materials into labeled target products, and can realize industrial production of isotope-labeled erythromycylamine. The method takes 13CD3 labeled methyl iodide as a starting raw material, the isotope-labeled erythromycylamine is synthesized by six steps of reactions, optimal preparation steps and reaction conditions arescreened out through a large number of experiments, the whole process is reasonable in design and high in operability, the labeled raw materials can be efficiently converted into labeled target products, the chemical purity of the labeled erythromycylamine prepared through the method can reach 98.5% or above, and the labeled isotope abundance is larger than 98.5%.
Macrolide derivative and application thereof
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Paragraph 0022; 0045, (2017/08/28)
The invention provides a macrolide derivative of a novel structure. Experiments show that the macrolide derivative has a good promoting effect on alimentary motility and is capable of enhancing intestine peristalsis, increasing defecation quantity and accelerating passing of intestinal content; on such basis, it is further discovered that the macrolide derivative is low in antibiotic activity and small in side effect and can be taken as a gastrointestinal motility promoting drug. Particularly, a compound III-3 screened with the optimal efficacy is subjected to further efficacy evaluation as well as acute toxicity and cardiotoxicity evaluation by domestic rabbits, beagles and marmosets. Experiments show that the compound III-3 is safe and capable of effectively promoting gastrointestinal motility, thereby being excellent in druggability.