Method for synthesizing ivermectin

A technology for ivermectin and avermectin, which is applied in the field of synthetic ivermectin, and can solve the problems of expensive rhodium catalysts and the like

Active Publication Date: 2014-07-16
河北美荷药业有限公司
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Problems solved by technology

[0005] The purpose of the invention is to solve the expensive defect of the existing rhodium catalyst, and provide a method for replacing the rhodium catalyst with a cheap catalyst to catalyze the hydrogenation of abamectin to synthesize ivermectin

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  • Method for synthesizing ivermectin
  • Method for synthesizing ivermectin
  • Method for synthesizing ivermectin

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Embodiment Construction

[0019] The present invention will be further described in detail below in conjunction with the embodiments.

[0020] The invention provides a method for synthesizing ivermectin. The method is catalyzed by ruthenium trichloride and monosulfonated triphenylphosphine sodium salt, avermectin and hydrogen are hydrogenated to obtain ivermectin .

[0021] Compared with rhodium, the price of ruthenium is only about 1 / 10 of that of rhodium, and the use of the catalyst of the invention can reduce the synthesis cost of ivermectin by about 30%.

[0022] Preferably, the molar ratio of the monosulfonated triphenylphosphine sodium salt to ruthenium trichloride (3-5):1.

[0023] Preferably, the mass ratio of ruthenium trichloride to abamectin is 1: (10-20).

[0024] Preferably, the hydrogenation reaction is carried out in a water-organic solvent two-phase system.

[0025] The water-organic solvent two-phase system refers to the mixture of water and organic solvent to form a liquid-liquid two-phase mixe...

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Abstract

The invention belongs to the field of veterinary drug synthesis and discloses a method for synthesizing ivermectin. In the method, under the catalysis of ruthenium trichloride and monosulfonated triphenylphosphine sodium salt, hydrogenation reaction occurs between abamectin and hydrogen to obtain ivermectin. Compared with the rhodium catalyst, the ruthenium trichloride used in the present invention is cheap, and can effectively reduce the production cost of abamectin hydrogenation to prepare ivermectin. The hydrogenation reaction is carried out in a water-organic solvent two-phase system, the separation of the catalyst, the reactant and the product is convenient, the catalyst is easy to recover, and at the same time, the residual amount of heavy metals in the product is reduced, and the cost of product purification is saved. The conversion rate of abamectin hydrogenation to synthesize ivermectin by adopting the method of the invention reaches 75%, and the selectivity reaches 77%, which is suitable for industrial application.

Description

technical field [0001] The invention belongs to the field of veterinary drug synthesis, and in particular relates to a method for synthesizing ivermectin. Background technique [0002] Ivermectin (IVM ) is a new type, broad-spectrum, efficient, and safe insecticide and acaricide. It is used in agricultural production to remove pests and mites from crops. In veterinary medicine, it is used to kill animals in vivo and in vitro Parasite, medically used in the treatment of human onchocerciasis. In the late 1980s, my country successfully developed ivermectin, and completed pharmacological and clinical treatment observations in accordance with the national second-class new drug. Ivermectin can be obtained by selective hydrogenation of avermectin. Abamectin is a group of sixteen ring lactone derivatives produced by Streptomyces. Its structural formula is as follows (when X is -CH=CH-, it is Abamectin; bacteria): [0003] [0004] It contains 5 carbon-carbon double bonds in i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/08C07H1/00B01J27/13
Inventor 孟凡桥高利华梁剑平陶蕾陈积红赵凤舞王曙阳
Owner 河北美荷药业有限公司
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