1100021-03-1

Basic information

• Product Name: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt
• Synonyms: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt
• CAS NO: 1100021-03-1
• Molecular Weight: 693.35
• Mol File: 1100021-03-1.mol

Chemical Properties

• CAS DataBase Reference: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt(1100021-03-1)
• EPA Substance Registry System: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt(1100021-03-1)

Safety Data

• Hazardous Substances Data: 1100021-03-1(Hazardous Substances Data)

Upstream product

• 100-46-9 benzylamine 
• 158966-92-8 montelukast 
• 287930-77-2 (S,E)-1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propan-1-ol 

Downstream Products

• 158966-92-8 montelukast 
• 151767-02-1 Montelukast sodium 

Relevant articles and documents

NOVEL MONTELUKAST 4-HALOBENZYLAMINE SALT AND METHOD FOR PREPARING MONTELUKAST SODIUM SALT BY USING THE SAME

Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. In Formula 2, X represents F, Cl, Br or I.

NOVEL MONTELUKAST 4-HALOBENZYLAMINE SALT AND METHOD FOR PREPARING MONTELUKAST SODIUM SALT BY USING THE SAME

Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. (Formular I and II should be inserted here) In Formula 2, X represents F, CI, Br or I.

METHOD FOR ISOLATION AND PURIFICATION OF MONTELUKAST

A method of isolation of Montelukast of formula I from reaction mixtures, comprising conversion of the crude sub-stance to well-crystallizing salts with primary amines in the environment of at least one organic solvent and acetonitrile, followed by re-crystallization of these salts with simultaneous removal of chemical impurities and use of the chemically pure salts of Montelukast with primary amines for direct transformation to the pharmaceutically useful amorphous form of Montelukast sodium of formula II.

SALTS OF MONTELUKAST AND PROCESS THEREFOR

The present invention relates to new salts (II) of Montelukast (I) and process for preparing these salts where B is ammonia, benzylamine or phenyl hydrazine. The invention also provides a process for preparation amine salts comprising (a) dissolving/ suspending the Montelukast free acid of formula (I) in an organic solvent (b) reacting with an amine (c) isolating the amine salt of formula (II) by adding optionally another anti-solvent, and (d) optionally drying the isolated solid under vacuum. The invention provides a process for preparation of sodium salt of montelukast acid comprising lowering pH of aqueous solution of amine salt of montelukast having formula II to 5.0±0.5, raising pH to above 8.0 using source of sodium ion, and isolating, the sodium salt by crystallization.