Argatroban byproduct and its synthesis, separation and identification method

A technology for argatroban and by-products, which is applied in the fields of argatroban by-products and synthesis and separation and identification, can solve the problems of difficult separation, difficult purification, and difficulty in reaching the standard of impurity content of product Argatroban, and achieves mild conditions and steps. Reasonable design and simple operation
CN101033223AActive Publication Date: 2007-09-12TIANJIN WEIJIE TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN WEIJIE TECH
Publication Date
2007-09-12

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Abstract

This invention relates to an outgrowth of argatroban and a method for synthesization and separation and authentication, in which, when preparing argatroban by catalysis and hydrogenation, it makes an outgrowth with difficult separation to determine that said outgrowth is a compound by separation, authentication and synthesization, which is hydrolyzed further to get argatroban, and when testifying the hydrolyzed intermediate, it first of all recovers nitro delinking, then hydrolyzes quinoline 1, 2, 3 and 4 to get 1, and the content of compound 3 can be reduced to the allowance sphere by following the hydrogenation reactin of the intermediate.
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Description

technical field

[0001] The invention relates to a by-product of argatroban and its synthesis, separation and identification method. technical background

[0002] In 1978, the antithrombin activity of argatroban (Argatroban, 1) hydrate [US 4 101 653] was first reported by S.Okamoto of Mitsubishi Chemical Company in Japan. During the following 20 years, many researchers conducted in-depth research on the biological activity of Argatroban and its value as medicine. In 1981, S.Okamoto compared heparin in animals [Okamoto, S.et al., Biochem.Biophys.Res.Commun.101, 440 (1981)]; T.Kumoto et al. Report [Kumada, T.et al., Thromb.Res.24, 285 (1981)]; In 1984, R.Kumao carried out clinical hemodialysis evaluation [Kikumoto, R.et al., Biochemistry 23, 85 (1984) ]; In 1986, the author reported that Argatroban inhibited thrombin activity in mammals, which can be used as a treatment and prevention agent for thrombosis and platelet aggregation inhibitor. Argatroban monohydrate can be used...

Claims

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