Preparation method and application of avermectin derivative

A kind of technology of avermectin and derivatives, applied in the directions of sugar derivatives preparation, sugar derivatives, sugar derivatives and the like

Inactive Publication Date: 2017-06-27
GUANGXI ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far, there have been no reports of applying abamectin derivatives obta...

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  • Preparation method and application of avermectin derivative
  • Preparation method and application of avermectin derivative
  • Preparation method and application of avermectin derivative

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Embodiment Construction

[0019] One, Abamectin derivative B of the present invention 1e preparation of

[0020] Fresh gorgonian coral (Anthogorgia caerulea) samples (wet weight about 5.0kg) were shredded and then soaked in ethanol and dichloromethane at room temperature, and then vacuum concentrated (0.09MPa, 43°C) to obtain a concentrated extract. The gorgonian concentrated extract is extracted with an equal volume of petroleum ether, and the extraction is repeated until the petroleum ether phase is colorless. The petroleum ether phase was discarded, the residual phase was first extracted with an equal volume of ethyl acetate, the obtained ethyl acetate phases were combined, and concentrated under reduced pressure to obtain 24.82 g of the ethyl acetate phase extract.

[0021] Mix 24.82g of ethyl acetate extract with silica gel powder evenly, put it into a normal phase silica gel column by wet packing, and use CHCl 3 -Me 2 CO system (CHCl 3 : Me 2 CO=1:0.1, 1:0.2, 1:0.4, 1:0.8 / V:V) Gradient eluti...

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Abstract

The invention discloses an avermectin derivative which is obtained by extracting and separating Anthogorgia caerulea and is named as 5-O-dimethyl-25-bis-(1-methyl propyl)-25-[(1S)-1,4-dimethyl amyl] abamectin Ala. The test shows that the EC50 value of the avermectin derivative B1e to resist adhering of typical marine fouling organism barnacle (0.12+-0.02 mu g/mL) is far smaller than the positive control butenolide (4.37+-1.22 mu g/mL), and the derivative has excellent activity to resist the typical marine fouling organism barnacle. The compound Ble is a marine natural active ingredient, is easily soluble in methanol and ethanol and has excellent alcohol-philicity, so that the avermectin derivative can be used separately or combined for preparing efficient marine anti-fouling paint. A new application is developed for the avermectin derivative, and a new source is provided for preparing the novel marine anti-fouling paint.

Description

technical field [0001] The invention belongs to the field of marine environmental protection and antifouling, and in particular relates to a preparation method and application of abamectin derivatives, in particular to a natural abamectin derivative derived from Gorgoniana genus in marine antifouling paints Applications. Background technique [0002] The attachment and accumulation of marine fouling organisms limit people's development and utilization of marine resources, such as accelerating the corrosion of metals, affecting the normal use of marine infrastructure, and causing serious damage to industries such as shipping, aquaculture, coastal defense, and coastal power plants. Technical and operational troubles. Biofouling is a serious global problem in marine ecosystems, resulting in increased material and economic costs worldwide. Commonly used chemical means to prevent the accumulation of fouling organic matter, such as various toxic substances (organotin compounds) ...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/08C09D5/16
CPCC07H1/08C07H17/08C09D5/1625
Inventor 高程海余练李菲何碧娟江蕾李家怡
Owner GUANGXI ACAD OF SCI
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