- METHODS FOR PREPARING SARPOGRELATE HYDROCHLORIDE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention provides hydrochloride salt hydrochloride. More specifically, the present invention relates to a method for preparing a hydrochloride salt having high purity and less toxicity in the body, and a pharmaceutical formulation comprising the same. The present invention relates to a hydrochloride and a pharmaceutical composition containing the same, and to a pharmaceutical composition containing the same, and a pharmaceutical composition containing the same, and a pharmaceutical composition containing the same. (by machine translation)
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Paragraph 0084; 0086-0090; 0158
(2020/10/20)
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- Crystallizine Sapogrelate Hydrochloride and a method for forming the same
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Disclosed are sarpogrelate hydrochloride crystals used an anticoagulant. A method to produce the sarpogrelate hydrochloride crystals by the present invention includes: a step of making 2-[2-hydroxy-3-dimethylaminopropoxy]-3andprime;-methoxybenzyl hydrochloride represented by chemical formula 3 react with succinic anhydride represented by chemical formula 4 in the presence of an organic base; a step of removing the hydrochloride of the generated organic base after completion of the reaction; and a step of adding aqueous hydrochloric acid solution to filtrate from which the hydrochloride of the organic base is removed. The sarpogrelate hydrochloride crystals include 60-80 wt% of sarpogrelate hydrochloride form I crystals and 20-40 wt% of sarpogrelate hydrochloride form II crystals. The present invention is able to solve the mixing problem of the sarpogrelate hydrochloride form II crystals.COPYRIGHT KIPO 2019
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Paragraph 0057; 0058
(2019/10/08)
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- Process for preparing sand Greythe ester is new hydrochloric acid
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The present invention discloses a preparation method of sarpogrelate hydrochloride. According to the preparation method, 2-[2-(3-methoxyphenyl)ethyl]phenol is adopted as a starting reactant, benzyl triethylammonium chloride is adopted as a phase transfer catalyst, the starting reactant, the phase transfer catalyst and epichlorohydrin form an ether in toluene and water, dimethylamine is adopted to carry out aminolysis in a pressurization reactor after the ether is formed to obtain 1-dimethylamino-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]-2-propanol, the 1-dimethylamino-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]-2-propanol and succinic anhydride are subjected to esterification in acetone, hydrogen chloride gas is directly introduced without recovery and replacement of the solvent to form a hydrochloride, and re-crystallization with acetone is performed to obtain the sarpogrelate hydrochloride refined product, wherein the purity is more than 99%.
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Paragraph 0019; 0023; 0027
(2018/07/10)
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- Syntheses and Platelet Aggregation Inhibitory and Antithrombotic Properties of ethyl>benzenes
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A series of ethyl>benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimantal thrombosis in mice.The results showed that the compounds were in vitro inhibitors of collagen-induced platelet aggregation.Most of them were also effective in the mouse antithrombotic assay.The compounds were found to be potent antagonists to S2 serotonergic receptor, and good correlation (r = 0.85) between their S2 serotonergic receptor antagonism and their potency as platelet antiaggregatory drugs was observed.Among the compounds studied, monophenoxy>methyl>ethyl>succinate hydrochloride (12b, MCI-9042) was selected for further pharmacological and toxicological evaluation.
- Kikumoto, Ryoji,Hara, Hiroto,Ninomiya, Kunihiro,Osakabe, Masanori,Sugano, Mamoru,et al.
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p. 1818 - 1823
(2007/10/02)
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- Pharmaceutically active (3-aminopropoxy)bibenzyl derivatives
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(3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.
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