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Method for synthesizing ivermectin

A technology of ivermectin and avermectin, applied in the field of synthesizing ivermectin, can solve problems such as expensive rhodium catalyst

Active Publication Date: 2013-11-13
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, which is used for obtaining ivermectin through hydrogenation reaction of the ivermectin and hydrogen gas under catalysis of ruthenium trichloride and mono-sulfonated triphenyl phosphine sodium salt. Compared with rhodium catalyst, the ruthenium trichloride used by the method for synthesizing ivermectin is low in price, and capable of effectively lowering the production cost of ivermectin which is prepared by hydrogenation of abamectin. The hydrogenation reaction is carried out in a water-organic solvent two-phase system, the catalyst is conveniently separated from reactant and the product, and is easy to recycle; meanwhile, the residual quantity of heavy metals in the product is lowered, and the cost during the product purification process is saved. Besides, the conversion rate for hydrogenation of the ivermectin by abamectin reaches 75%, the selectivity reaches 77%, and therefore, the method 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...

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Application Information

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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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