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Preparation and application of macrolide compound

A technology of macrolide and compound is applied in the field of preparation of macrolide compound to achieve the effect of low toxicity agricultural insecticidal and acaricidal activity

Active Publication Date: 2014-12-24
NANKAI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Very hydrophilic drugs cannot pass through the lipid layer of the biomembrane, while very hydrophobic drugs remain as part of the biomembrane for similar and compatible reasons, so they cannot effectively enter the inner cytoplasm

Method used

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  • Preparation and application of macrolide compound
  • Preparation and application of macrolide compound
  • Preparation and application of macrolide compound

Examples

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Synthetic example

[0031] Preparation of intermediate 15-O-p-nitrophenyl carbonate ivermectin B1a

[0032] Add dry ivermectin B1a15.63g (18mmol) to a 250ml round bottom flask, dissolve in 150ml tetrahydrofuran, and add 2.09g (18mmol) tetramethylethylenediamine dropwise in an ice-salt bath. After stirring for 10 minutes, add 7.21g (36mmol) p-nitrophenyl chloroformate, and after the system turns into a brown turbid system, remove the ice-salt bath and change to stirring at room temperature. TLC followed the reaction until the raw material point did not change and then stopped stirring. The insoluble matter was removed by suction filtration, and the filtrate was rotary evaporated to remove tetrahydrofuran to obtain a yellow solid. 150ml of dichloromethane was added to the obtained solid to obtain a brown turbid system, which was washed with water (60ml×3) and then washed once with saturated brine. After drying the organic phase with anhydrous sodium sulfate, the solvent was removed to obtain a cr...

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Abstract

The invention relates to a macrolide compound as well as a preparation method and application thereof, in particular a modified ivermectin derivative as well as a preparation method and application thereof. General formulas (I) (II) of the compound of the macrolide derivative and salt thereof are as shown in the specification. The compound disclosed by the invention is efficient, safe, stable, wide in spectrum and low in toxicity, and has an excellent agricultural insecticidal and acaricidal activity as well as an activity of killing parasites of domestic animals and medical uronema, wherein n represents 0, 1, 2, 3, 4, 5, 6 or 7; X is either N or O; Y represents Cl<->; Z is either N or O; R1 and R2 are selected from H and C1-C4 alkyl; or ZR1R2 is selected from the following structures as shown in the specification.

Description

Technical field: [0001] The invention relates to the preparation of a macrolide compound, in particular to a modified ivermectin derivative, a preparation method thereof, and an application in the prevention and treatment of agricultural pests and livestock parasites and in clinical medicine. Background technique: [0002] So far, the typical commercialized varieties of macrolide as the activator of chloride ion channel have abamectin (abamectin), ivermectin (Ivermectin), emamectin benzoate (emamectin benzoate). ) and mi lbemectin (mi lbemectin) and so on. [0003] Abamectin is a sixteen-membered macrolide diglycoside compound. It is a broad-spectrum insecticide and acaricide. Its insecticidal spectrum has more than 80 species, which can effectively control Diptera, Homoptera, Coleoptera and Lepidoptera pests and many kinds of harmful mites. The control spectrum is very wide, and it has the functions of killing insects, killing acarids and killing nematodes, and is often ...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/00A61K31/7048A61K31/706A61K31/7056A61P33/10A01N43/90A01P7/04A01P7/02
Inventor 邹小毛傅翠蓉臧福坤李引红单鹏程刘俊黄纯王鑫杨亚哲李永强
Owner NANKAI UNIV
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