Synthetic method of argatroban and intermediate thereof

A technology of argatroban and intermediates, applied in the field of drug synthesis, which can solve the problems of difficult removal of water
CN101348463AActive Publication Date: 2009-01-21天津药物研究院药业有限责任公司 +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
天津药物研究院药业有限责任公司
Publication Date
2009-01-21

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Abstract

The invention relates to a method for preparing N<2>-(3-methyl-8-quinoline sulfonyl)- N-nitryl-L-arginine as the intermediate of argatroban. The method comprises the following steps that the reaction of N-nitryl-L-arginine and a 3-methyl-8-quinoline sulfonyl chloride-THF solution is carried out in an aqueous solution of sodium carbonate ; after the reaction ends, THP is collected through evaporation, and the water layer is extracted with an organic solvent, then THF is added with pH adjusted to 2-3, and then a solid saturated water layer of inorganic salt is added; THF is separated and a desiccant is added and stirred for 10-24 hours, with water content of THF measured to be less than 1 percent, then a molecular sift is added for drying, with the water content of THF controlled within 0.2 percent, and then THF reacts with (2R, 4R) 4MPE directly. The invention solves well the control on the water content of N<2>-(3-methyl-8 quinoline sulfonyl)-N N-nitryl-L-arginine, ensures the successful implementation of amide acylation, and satisfies the requirement of the large-scale industrial production.
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Description

technical field

[0001] The present invention relates to the technical field of medicine synthesis, more specifically, argatroban intermediate N 2 -(3-Methyl-8-quinolinesulfonyl)-N G - Process for the preparation of nitro-L-arginine. Background technique

[0002] Acute and ischemic stroke are the five most common diseases in the world, and stroke mortality accounts for 10-12% of the total death toll. Survivors after stroke account for 75% of stroke patients and most of them have sequelae, such as common language, sensory or motor dysfunction, requiring long-term hospitalization and family care, which brings serious economic problems to society and families, and is even more serious patients can be life-threatening. In my country, about 3 million people suffer from stroke every year, and it is on the rise in recent years, and there is a lack of acute treatment drugs.

[0003] Argatroban (Argatroban) is the only synthetic drug approved for the treatment of acute ischemic st...

Claims

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