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Method for preparing moxidectin

An allyloxycarbonyl and oxo technology, applied in the field of preparation of new antiparasitic drugs, can solve problems such as affecting product quality and yield, and achieve the effects of sufficient supply, mild reaction conditions and simple process

Active Publication Date: 2020-08-28
JIANGSU WEI LING BIOCHEM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Seriously affect the quality and yield of the product

Method used

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  • Method for preparing moxidectin
  • Method for preparing moxidectin

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Experimental program
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Embodiment 1

[0047] A. Preparation of 5-oxo(allyloxycarbonyl)nimoctin (Ⅱ)

[0048] Add nimoctine (613g, 1.0mol), imidazole (613g) and dichloromethane (3050g) into the reactor, stir well and cool to -5 to 5°C, then add allyl chloroformate dropwise under stirring (132.5g, 1.1mol) and dichloromethane (600g) mixed solution, keep the temperature of the mixture not exceeding 5°C during the dropwise addition, keep -5 to 5°C after the dropwise addition, continue to stir and react for 8 hours, and naturally rise after the reaction to room temperature, the mixture was washed with saturated brine, the organic phase was dried with anhydrous sodium sulfate after separation, the filtrate was filtered to remove the desiccant, and the filtrate was concentrated to obtain an oil, and the oil was recrystallized with methanol (2000g) to obtain 5- Oxy(allyloxycarbonyl)nemoctine (Ⅱ), 683.1g of light yellow powder, yield about 98.0%, HPLC detection is consistent with the standard comparison, content greater than...

Embodiment 2

[0056] Other steps are identical with embodiment 1, just the preparation method of the 5-oxygen (allyloxycarbonyl) nimoctine (II) of A step is as follows:

[0057] Add nimoctine (613g, 1.0mol), imidazole (367.8g) and dichloromethane (1250g) into the reactor, stir well and cool to -5 to 5°C, then add allyl chloroformate dropwise under stirring A mixed solution of ester (120.5g, 1.0mol) and dichloromethane (600g), keep the temperature of the mixture not exceeding 5°C during the dropwise addition, and keep stirring at -5 to 5°C after the dropwise addition for 4 hours. Rising to room temperature, the mixture was washed with saturated brine, the organic phase was dried with anhydrous sodium sulfate after separation, the filtrate was filtered to remove the desiccant, and the filtrate was concentrated to obtain an oily substance, which was recrystallized with methanol (1800g) to obtain 5 -Oxy(allyloxycarbonyl)nemoctine (Ⅱ), 534.6g of light yellow powder, yield about 77.0%, HPLC detec...

Embodiment 3

[0059] Other steps are identical with embodiment 1, just the preparation method of the 5-oxygen (allyloxycarbonyl) nimoctine (II) of A step is as follows:

[0060] Add nimoctine (613g, 1.0mol), imidazole (490g) and dichloromethane (2200g) into the reactor, stir well and cool to -5 to 5°C, then add allyl chloroformate dropwise under stirring (126.5g, about 1.05mol) and dichloromethane (600g) mixed solution, keep the temperature of the mixture not exceeding 5°C during the dropwise addition, keep -5 to 5°C after the dropwise addition and continue to stir the reaction for 6 hours. Rising to room temperature, the mixture was washed with saturated brine, the organic phase was dried with anhydrous sodium sulfate after separation, the filtrate was filtered to remove the desiccant, and the filtrate was concentrated to obtain an oil, and the oil was recrystallized with methanol (2500g) to obtain 5 -Oxy(allyloxycarbonyl)nemoctine (II), 608.5g of light yellow powder, yield about 87.3%, HP...

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Abstract

The invention discloses a method for preparing moxidectin. The method sequentially comprises the following steps: with nemadectin is used as a raw material performing substitution, oxidization and de-protection reactions on allyl chlorocarbonate; The invention discloses a novel synthesis route, wherein used raw materials have characteristics of wide and sufficient source; the method has advantagesof proper cost, simple process, mild reaction conditions of each step, conventional operation, and production cost reducing.

Description

technical field [0001] The invention relates to a preparation method of a new antiparasitic drug, in particular to a method for preparing moxidectin. Background technique [0002] In the process of raising livestock and poultry, livestock and poultry are easily infected by parasites and cause a series of diseases. Severe cases may cause plague, which is very destructive to the entire animal husbandry industry. Studies in recent years have shown that the global animal husbandry industry attaches great importance to the field of anti-parasites, and new drugs and new processes are constantly emerging, and anti-parasitic veterinary drugs are also widely used in animal husbandry. [0003] Moxidectin, also known as moxidectin, is a new type of antiparasitic drug. It is a single-component macrolide antibiotic fermented by Streptomyces. It is produced internationally by Novartis of Switzerland and Sankyo of Japan. It was discovered in 1967 by Japan's Sankyo Company in the screening...

Claims

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Application Information

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IPC IPC(8): C07D493/22
CPCC07D493/22Y02P20/55
Inventor 凌青云蒋忠良张猛李惠娟
Owner JIANGSU WEI LING BIOCHEM TECH CO LTD
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