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Acetyl isovaleryl tylosin amide, preparation method and application

A technology of acetylisovaleryl tylosin amine and compound, which is applied in the field of novel acetylisovaleryl tylosin amide, and achieves the effects of simple preparation method, mild conditions and high yield

Active Publication Date: 2013-04-24
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no literature reports on the synthesis and application of acetylisovaleryl tylosin C-20 carbonyl reductive amination derivatives. The present invention modifies acetylisovaleryl tylosin to synthesize acetylisovaleryl tylosin Derivatives of the basic structure of acyltylosin, the study of its anti-mycoplasma and antibacterial activity is of great significance for further research on new anti-mycoplasma and antibacterial drugs, and the development of drugs with independent intellectual property rights

Method used

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  • Acetyl isovaleryl tylosin amide, preparation method and application
  • Acetyl isovaleryl tylosin amide, preparation method and application
  • Acetyl isovaleryl tylosin amide, preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Example 1: Preparation formula 2 Shown-NR 1 R 2 =-N(C 2 h 5 ) 2 Derivatives( 2-a )

[0038] take compound 1 (416mg, 0.4mmol), diethylamine (62μl, 0.6mmol) was dissolved in 5ml of methanol, after heating to 40°C, formic acid (31μl, 1.5mmol) was added, after constant temperature reaction for 8h, after the system was concentrated, 20ml of water was added Dissolve the residue, then adjust the pH with aqueous sodium hydroxide solution until no precipitation occurs, then filter with suction, dry and weigh the filter cake to obtain the compound 2-a (350mg), yield 80.61%, off-white solid.

Embodiment 2

[0039] Example 2: Preparation formula 2 Shown-NR 1 R 2 =-N(n-C 4 h 9 ) 2 Derivatives( 2-b )

[0040] take compound 1 (416mg, 0.4mmol), di-n-butylamine (101μl, 0.6mmol) was dissolved in 5ml of methanol, after heating to 60°C, sodium borohydride (23mg, 1.5mmol) was added, and after constant temperature reaction for 8h, the system was concentrated, Add 20ml of water to dissolve the residue, then adjust the pH with aqueous sodium hydroxide solution until no precipitation occurs, then filter with suction, dry and weigh the filter cake to obtain the compound 2-b (320mg), yield 70.08%, off-white solid.

Embodiment 3

[0041] Embodiment 3: Preparation formula 2 Shown-NR 1 R 2 =-NC 5 h 10 (tetrahydropyrrolyl) derivatives ( 2-d )

[0042] take compound 1 (416mg, 0.4mmol), tetrahydropyrrole (50μl, 0.6mmol) was dissolved in 5ml ethanol, after heating to 60°C, formic acid (31μl, 1.5mmol) was added, after constant temperature reaction for 8h, the system was concentrated, and 20ml of water was added Dissolve the residue, then adjust the pH with aqueous sodium hydroxide solution until no precipitation occurs, then filter with suction, dry and weigh the filter cake to obtain the compound 2-d (300mg), yield 69.22%, off-white solid.

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Abstract

The invention belongs to the field of medicinal chemistry and discloses an acetyl isovaleryl tylosin amine derivative with anti-mycoplasma and antimicrobial activity, a synthesis method and an application thereof. The preparation method of the compound disclosed by the invention is simple, mild in condition, and high in yield. An external activity test proves that the acetyl isovaleryl tylosin amide provided by the invention has an obvious inbibitional effect on animal mycoplasma and G+, G- infection, and can be applied to the preparation of anti-mycoplasma and antimicrobial drugs.

Description

technical field [0001] The invention relates to a novel acetylisovaleryl tylosin aminate, a synthesis method and application thereof, and belongs to the field of medicinal chemistry. Background technique [0002] Acetylisovaleryl Tylosin (1) is a brand-new macrolide antibiotic commercialized by the British Yike Animal Health Products Co., Ltd. It acetylates the 3-position and 4-position of Tylosin through microbial transformation. The macrolide animal-specific antibiotics obtained by isovalerylation have been approved and sold in many countries; it is currently the most sensitive drug to mycoplasma in the world, and it is a good solution to the problem with macrolides. and other types of drugs, cross-resistance and residue problems, the drug effect is significantly higher than tylosin; Bacillus etc. have inhibitory effect. However, there are no literature reports on the synthesis and application of acetylisovaleryl tylosin C-20 carbonyl reductive amination derivatives. The...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H17/00C07H1/00A61K31/7048A61K31/7056A61K31/706A61P31/04A61P29/00
Inventor 施秀芳邱启平姚海峰孙帅军由丹
Owner ZHENGZHOU UNIV
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