- Synthesis and purification method of tildipirosin
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The invention discloses a synthesis and purification method of tildipirosin. The method comprises the following steps of dissolving tylosin phosphate in an organic solvent, adding formic acid and piperidine, and performing a heating reaction; performing cooling, adding water and hydrobromic acid, and performing standing for layering; hydrolyzing an aqueous solution A, performing cooling, adding the organic solvent, and performing standing for layering; adding alkali into a water phase to adjust the pH value to 6.5-7.0, adding the organic solvent and alkali to adjust the pH value to be greater than 13, performing standing for layering to obtain a filtrate, and controlling the water content to be less than 0.1% through atmospheric distillation; adding triphenylphosphine and pyridine, performing heating, dropwise adding an iodine solution, continuously reacting, performing cooling, adding alkali for quenching, and performing standing for layering; adding an alkali catalyst and piperidine into the filtrate C, performing a heating reaction, performing cooling, adding acid to adjust the pH value to 6.20-6.80, and performing standing for layering; adding the organic solvent into the water phase, and performing standing for layering; and continuously adding the organic solvent and the alkali into the water phase to adjust the pH value to be greater than 13, and performing standing for layering to obtain a filtrate D. The method is simple to operate, mild in reaction condition, low in cost and high in product yield, and the purity and content of the obtained tildipirosin are both greater than 99%; and the method is beneficial to industrial production.
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Paragraph 0042; 0044; 0048; 0050; 0054; 0056
(2021/04/21)
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- Novel 16-member triamilide derivatives and uses thereof
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The invention discloses 20,23-modified novel derivatives of 16-membered demycarosyltylonolide antibiotics, which are useful against bacterial and mycoplasmic pathogens in humans and animals. Also claimed are pharmaceutical compositions of such derivatives and their use in treating bacterial and mycoplasmic infections in humans and animals.
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Page/Page column 0072-0073
(2018/06/09)
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- Sixteen membered ring triamine lactone derivatives and use thereof
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The invention discloses a novel sixteen-membered cyclotriaminolactone derivative and application thereof. The novel sixteen-membered cyclotriaminolactone derivative is a compound represented by the formula (I) or formula (II) or a pharmaceutically acceptable salt thereof, wherein R1 Is an optionally substituted C1-6 alkyl group or C3-8 cycloalkyl group, R2 is hydrogen, an optionally substituted C1-6 alkyl group or C3-8 cycloalkyl group, or R1 and R2 are chemically bonded to each other so that R1-N-R2 group constitutes an optionally substituted three-five-membered or seven-nine-membered heterocyclic group, and R3 and R4 are each independently selected from hydrogen or a C1-3 alkyl group. The compound or the pharmaceutically acceptable salt thereof disclosed by the invention has excellent antibacterial activity and is useful for treating and preventing bacterial infections and mycoplasma infections in animals, and provides a new way for treating and preventing such diseases.
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Paragraph 0078; 0079
(2018/08/03)
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- MACROLIDE SYNTHESIS PROCESS
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This invention relates to a method for making macrolides, and, in particular, to a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl- tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides.
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Page/Page column 53-54
(2008/06/13)
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