- Process for Preparing Nafamostat Mesilate and Intermediate Thereof
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The present invention provides a method for efficiently producing astaxmostat mesylate through a simple process and a method for producing 6 - amidino -2 - naphthol mesylate in high yield under mild conditions.
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- Production of [...] acid salt
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The purpose of the present invention is to provide a process for producing nafamostat mesylate without via nafamostat bicarbonate and while avoiding inclusion of sodium mesylate. The process for producing nafamostat mesylate comprises (1) a step in which an anion-exchange resin in which the anion is a mesylic acid ion is prepared, (2) a step in which the anion-exchange resin obtained in the step (1) is brought into contact with a nafamostat salt which is neither nafamostat bicarbonate nor nafamostat mesylate, in the presence of a solvent to thereby convert the nafamostat salt into nafamostat mesylate by salt exchange, and (3) a step in which the nafamostat mesylate obtained in the step (2) is crystallized.
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Paragraph 0030; 0031; 0032
(2018/05/03)
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- Method for preparing of nafamostat mesilate
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The present invention discloses a manufacturing method for nafamostat mesylate used as blood coagulation inhibitor where crystalline II type nafamostat mesylate is obtained with high purity and quality as well as regularity. According to the present invention, the manufacturing method for nafamostat mesylate comprises the following steps of: (a) initiating a chemical reaction between 4-guanidino benzoic acidic hydrochloride and 6-amidino-2-naphthol methanesulfonate with the existence of N,N′-Diisopropylcarbodiimide to manufacture the compound shown in Formula 1; (b) adding the manufactured compound in Formula 1 to solvent mixed with water H_2O and saturated sodium hydrogen carbonate NaHCO_3 to manufacture the compound shown in Formula 2; and (c) adding the compound in Formula 2 to solvent, and then adding methanesulfonate to manufacture the nafamostat mesylate compound shown in Formula 3.
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Paragraph 0054; 0055
(2017/01/12)
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- AMIDINE COMPOUND
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Amidino compounds represented by the formula STR1 and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula STR2 with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceuticlly acceptable acid addition salts thereof.
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