cas 82957-06-0, 6-Amidino-2-naphthol methanesulfonate | Articles data ｜lookchem

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82957-06-0

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Process for Preparing Nafamostat Mesilate and Intermediate Thereof
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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(2021/10/27)

Methanesulfonic acid the naphthalene not takes charge of he intermediate — 6 - amidino - 2 - naphthol armor sulfonate synthetic method
The present invention relates to a new synthesis method for a nafamostat mesylate intermediate 6-amidino-2-naphthol methanesulfonate. According to the new method, 6-hydroxy-2-naphthaldehyde is adopted as a raw material, dimethyl sulfoxide is adopted as a reaction solvent, the dimethyl sulfoxide and hydroxylamine hydrochloride are subjected to an addition elimination reaction to obtain 6-cyano-2-naphthol, the 6-cyano-2-naphthol is subjected to a pinner reaction in a HCl/methanol solution to obtain 6-hydroxy-2-naphthalene imino methyl ester hydrochloride, ammonia gas is introduced to carry out an aminolysis reaction to obtain 6-amidino-2-naphthol, and the 6-amidino-2-naphthol sequentially reacts with sodium bicarbonate and methanesulfonic acid to convert into the 6-amidino-2-naphthol methanesulfonate. According to the present invention, in the new synthesis method, the 6-cyano-2-naphthol preparation in the first step adopts the completely-new method, the use of the highly toxic copper cyanide in the traditional method is avoided, the operations are simple, and the conditions are mild; and the second step adopts the improved pinner method, wherein the reaction of acetyl chloride and methanol is adopted to produce HCl to replace direct introduction of HCl gas into the reaction system, such that the improved method has strong operability and industrialization is easily achieved.
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Paragraph 0010; 0011; 0012; 0013

(2017/12/30)

Synthesis and structure-activity study of protease inhibitors. IV. Amidinonaphthols and related acyl derivatives
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Aoyama,Okutome,NakayamaT.,Yaegashi,Matsui,Nunomura,Kurumi,Sakurai,Fujii
p. 1458 - 1471
(2007/10/02)

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Chemical Properties

Melting Point: −100°C(lit.)
Boiling Point: 142-149°C(lit.)
Flash Point:75°F
Density: 0.876g/mLat 25°C(lit.)
Solubility:Acetonitrile (Slightly), DMSO (Slightly)
Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
PSA: 132.85000
LogP: 3.21430

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