Process for preparing argatroban hydrate

A technology of argatroban and hydrate, which is applied in the field of preparation of argatroban hydrate, can solve problems such as nonconformity, low yield, and large ratio change, and achieve mild operating conditions, high yield, and high product quality. high effect
CN100427480CActive Publication Date: 2008-10-22TIANJIN WEIJIE TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
TIANJIN WEIJIE TECH
Publication Date
2008-10-22

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Abstract

The invention discloses a preparing method of Argatroban hydrate, which comprises the following steps: refluxing Argatroban and water for 0.5-1.0h; dissolving; cooling to indoor temperature; evolving white crystal; filtering; washing twice; drying to obtain medical Argatroban hydrate. The invention guarantees the constant rate of R and S without other organic impurity, which improves hydrating receiving rate between 90% and 95%.
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Description

technical field

[0001] The invention relates to a preparation method of argatroban hydrate. technical background:

[0002] In 1978, the antithrombin activity of argatroban (Argatroban) hydrate was first reported by S.Okamoto of Japan Mitsubishi Chemical Company [US 4 101 653]. 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. Reported [Kumada, T.et al., Thromb.Res.24, 285 (1981)]; In 1984, R.Kumato 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 as a selective antithrombotic agent to tr...

Claims

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