Argatroban separation method

A technology for the separation of argatroban and its separation method, which is applied in the field of separation of the optical isomer compound argatroban, and can solve problems such as difficult separation, small separation amount, and many reaction by-products
CN100586946CActive Publication Date: 2010-02-03TIANJIN 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
2010-02-03

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Abstract

The invention discloses a separating method of optically-active pure isomer 21 (S)-Argatroban, which comprises the following steps: adopting 21(S) and 21(R) Argatroban as raw material; heating to reflux based on mixture of alcohol and water as solvent for 5-10h; cooling; stewing; filtering; obtaining white crystal product; drying; repeating 2-6 times; combining mother liquid; stripping solvent; detecting the content of 21 (S) through high-effect liquid-phase chromatography not less than 98%.
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Description

technical field

[0001] The invention relates to a method for separating optical isomer compound Argatroban (Argatroban), in particular to a method for separating pure 21(S)-argatroban. Background technique

[0002] In 1978, S.Okamoto of Mitsubishi Chemical Company in Japan firstly reported the antithrombin activity of Argatroban (Argatroban) monohydrate [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. Report [Kumada, T.et al., Thromb.Res.24, 285(1981)]; In 1984, R.Kumato conducted clinical hemodialysis evaluation [Kikumoto, R.et al., Biochemistry23, 85(1984)] ; In 1986, the author reported that Argatroban inhibited the thrombin activity in mammals, and could be used as a treatment and prevention agent for thrombosis and an inhibitor of pl...

Claims

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