Synthesis of tulathromycin

A technology of telamycin and its compound, which is applied in the field of synthesis of telamycin, achieves good industrialization prospects and shortens the reaction time

Pending Publication Date: 2021-12-31
江苏君若药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The reaction conditions only use 10 times the equivalent of n-propylamine, but the react

Method used

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  • Synthesis of tulathromycin
  • Synthesis of tulathromycin
  • Synthesis of tulathromycin

Examples

Experimental program
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Example Embodiment

[0021] Example 1: Preparation of taramromycin

[0022] (2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R) -2-ethyl-3, 4, 10-trihydroxy-13 - [[3S, 4S, " 6R, 8R] -8-methoxy-4,8-dimethyl-1,5-dioxidoid [2,5]-辛 -6-yl] oxygen group) 3, 5, 8, 10, 12,14-Sixththyl-11 - [[3,4,6-triode oxygen-3- (dimethylamino) -β-D-hexyloglycan group] oxygen group] -1-oxygen- 6-nitrogen heterocyclic dethylsnexane-15-ketone hydrate (compound formula I) (110 g, 143.8 mmol) and isopropanol (500 mL), stirred at room temperature and dissolved. Positive propylamine (12.75 g, 215.7 mmol, 1.5 eq) and trifluoromethanesulfonic acid (8.9 g, 14.4 mmol, 0.1 eq) were then added to the reaction system. After the addition is completed, the system was heated to 50 ° C for 3 hours. After the reaction is complete, the system is concentrated in vacuo to remove the organic solvent, add DMF (450 mL) to the residue, heat dissolved at 80 ° C, filtrate heat, stirring, the filtrate is slowly reduced to 5 ° C, stirred, stirred for 2 hours...

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Abstract

The invention relates to synthesis of tulathromycin, in particular to a reaction of (2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R)-2-ethyl-3, 4, 10-trihydroxy-13-[[3S, 4S, 6R, 8R]-8-methoxy-4, 8-dimethyl-1, 5-dioxaspiro [2, 5] oct-6-yl] oxy) 3, 5, 8, 10, 12, 14-hexamethyl-11-[[3, 4, 6-trideoxy-3-(dimethylamino)-beta-D-xylopyranosyl] oxy]-1-oxa-6-azacyclopentadecane-15-one monohydrate with n-propylamine in the presence of a solvent and ytterbium trifluoromethanesulfonate, so as to realize the synthesis of tulathromycin.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, in particular to the synthesis of telamycin. Background technique [0002] Tulathromycin (Tulathromycin), also known as tulathromycin, tolamycin, trade name "Draxxin" (Chinese name is "Rui Kexin" or "Rui Kexin"). The drug is a new type of erythromycin synthetic veterinary drug researched and developed by Pfizer Animal Health in the late 1990s. It is a semi-synthetic macrolide antibiotic for animals and is mainly used to treat and prevent animal diseases. Respiratory diseases caused by Actinobacillus pleuropneumoniae, Mycoplasma, Pasteurella, Haemophilus para, Bordetella bronchiseptica, etc. A large number of studies have found that Tyramycin can selectively penetrate Gram-negative bacterial pathogens and is used for the treatment of respiratory infectious diseases caused by sensitive bacteria in cattle and pigs and bovine infectious keratitis caused by Moraxella bovis. prevention. The drug wa...

Claims

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Application Information

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IPC IPC(8): C07H17/00C07H1/00
CPCC07H17/00C07H1/00
Inventor 朱灿杨晓瑜裔明月刘洁姜军
Owner 江苏君若药业有限公司
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