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Nafamostat mesylate

Nafamostat mesylate structure

CAS No:
82956-11-4
Formula:
C19H17N5O2.2CH4O3S
Chemical Name:
Nafamostat mesylate
Synonyms:
Benzoic acid,4-[(aminoiminomethyl)amino]-,6-(aminoiminomethyl)-2-naphthalenyl ester,methanesulfonate (1:2);Benzoic acid,4-[(aminoiminomethyl)amino]-,6-(aminoiminomethyl)-2-naphthalenyl ester,dimethanesulfonate;FUT 175;Nafamostat mesylate;Nafamostat mesilate;6-Amidino-2-naphthyl p-guanidinobenzoate;Futhan;Nafamostat dimethanesulfonate;Nafamastat mesylate;Coahibitor
Categories:
Biochemical Engineering > Inhibitors

Description

Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant.Target: Serine ProteaseTranilast (FUT-175) is an antiallergic drug for bronchial asthma. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis. It has also been investigated for use as an antiproliferative drug on drug-eluting stents.A 20-40 mg/h dose of FUT-175 prolonged coagulation time sufficiently in the instrumental blood of the extracorporeal ci

Nafamostat mesylate Basic Attributes

Molecular Weight：

539.58

Exact Mass：

539.114

EC Number：

1806241-263-5

HScode：

29252900

Characteristics

PSA：

266

Melting Point：

217-220 °C

Boiling Point：

637.2°C at 760 mmHg

Flash Point：

339.1ºC

Storage Conditions：

room temp

Toxicity：

Oral-rat LD50: 3050 mg/kg; Oral-Mouse LD50: 4600 mg/kg

Flammability characteristics：

Flammable; burning produces toxic nitrogen oxides and sulfur oxide fumes

Safety Information

Transport codes：

3077

wgk germany：

nwg

RTECS Number：

DG2736000

Storage features：

Warehouse ventilated, low temperature and dry

Precautionary statement(s)：

P281

Hazard Statements：

H361fd

Toxicity

Toxicity class：

moderately toxic

Nafamostat mesylate Use and Manufacturing

Methods of Manufacturing

At room temperature25.94 g of 4-guanidinobenzoic acid hydrochloride (4-GDA.HCl) was added to 207.5 ml of pyridine solvent, 18.6 ml of N, N'-diisopropylcarbodiimide (DIC) was added and reacted. to the next, to the reaction solution comprising the above reaction, 28.3 g of 6-amidino-2-naphthol methanesulfonate (6-ANL.MsOH) and 122 mg of 4-dimethylaminopyridine (DMAP) The mixture was stirred overnight at the same temperature as that of the reaction. next, methanol (MeOH) (69.3 ml) was added to the reaction mixture which had been stirred, stirred for 1 hour, filtered, Subsequently, the compound of Formula 1 purified by a purity of 99percent by a further purification process, in that not dry, saturated sodium in 233.28 ml of water (H2O) and 92.73 ml for 1 hour at a temperature of 25 ° C bicarbonate (NaHCO3) is added slowly to a mixed solution (solvent), and the crystal precipitates and stirred, after it was filtered, using a water and acetone by washing sequentially, the compound (purity according to the general formula (2): 98.9percent ) was prepared. To the next, the compound of formula (2) Without drying, after the mixture was dispersed in 72.87 ml of methanol while maintaining the temperature at room temperature, 9.3 ml of methanesulfonic acid (MsOH) was slowly added, The mixture was continuously stirred until no gas was generated. Then, it was cooled to 15 DEG C, After stirring for 10 minutes at the same temperature, the resulting solid was filtered, Washed sequentially with methanol and acetone, By hot air drying at a temperature of 50°C, by drying (Purity: 99.1percent, yield: 62.78percent) of the nafamostat mesilate according to the above formula (3).29.26 g (2.3 equivalents based on nafamostat hydrochloride described below) of a strong ionic exchange resin substituted with hydroxide ion was filled in a glass column (inner diameter: 0.8 - 0.9 cm, height: 6 cm), washed with water, then passed through a solution of 18.5 ml of methane sulfonic acid diluted with 288 ml of water, and methanesulfonated and washed with 160 ml of 50 vol percent aqueous acetone solution. Separately, 200 ml of water and 200 ml of acetone were added to 10.3 g of Nafamostat hydrochloride (net amount 8.0 g, HPLC purity: 99.8percent) to prepare a solution having a nafamostat conversion concentration of 1.8percent, then 3.8 ml of 1.0 mol / L methanesulfonic acid aqueous solution was added to adjust the pH to 2.0. The nafamostat solution was passed through the above-said column and washed with 160 ml of 50 vol percent aqueous acetone solution. Only fractions containing Nafamostat were combined (341 g) and 736 ml of acetone was added to this solution while stirring at 8 ° C and nafamostat mesilate/mesylate were added as seed crystals. Further, 1288 ml of acetone and 16 ml of water were added. The precipitated crystals were filtered over 20 minutes with Kiriyama funnel having an inner diameter of 60 mm and dried to obtain 8.81 g of nafamostat mesylate (HPLC purity: 99.9percent, residual chloride ion: 0.007percent).

Uses

Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma

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