869066-93-3

Upstream product

• 181139-72-0 methyl-[(E)]-2-[3(S)-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-hydroxypropyl] benzoate 
• 149968-11-6 methyl 2-(3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-oxopropyl)benzoate 
• 108-24-7 acetic anhydride 
• 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

• 1197374-09-6 (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyl)propyl acetate 
• 1266620-74-9 [R,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl]-3-[2-(hydroxy-1-methylethyl)phenyl]propyl]-sulfonyl]methyl]-cyclopropane acetic acid 
• 855473-51-7 1-(((1(R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid methyl ester 
• 918972-54-0 [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-[1-(1-methyl)ethenyl]phenyl]propyl]thio]methyl]cyclopropaneacetic acid 
• 1334676-80-0 [R,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[(prop-1-en-2-yl)phenyl]propyl]thio]methyl]cyclopropane acetic acid methyl ester 
• 1351973-25-5 [R,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-methoxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropane acetic acid 
• 1197374-11-0 (S)-1-(3-((E)-2-(7-chloroquinolin?2-yl)vinyl)phenyl)-3-(2-isopropenylphenyl)propyl methanesulphonate 
• 1352029-52-7 1R-{(3-[(E)-2-(7-chloroquinolin-2-yl) vinyl] phenyl)}-3-[2-(prop-1-en-2-yl) phenyl] propan-1-ol 
• 1351973-21-1 [S,E]-1-[[[1-[3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl]-3-[2-(prop-1-en-2-yl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid 
• 1351973-22-2 [S,E]-1-[[[1-[3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl]-3-[2-(prop-1-en-2-yl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid dicyclohexylamine salt 
• 1197374-12-1 [1-[(R)-1-(3-[(E)-2-(7-chloroquinolin-2-yl)vinyl]-phenyl)-3-(2-isopropenylphenyl)propylsulfanylmethyl]cyclopropyl]acetic acid dicyclohexylamine salt 
• 190078-45-6 [S,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropane acetic acid sodium salt 
• 220927-27-5 (R,E)-(1-{1-{3-[2-(7-Chloroquinolin-2-yl)ethenyl]phenyl}-3-[2-(1-hydroxy-1-methylethyl)phenyl]propylsulfanylmethyl}cyclopropyl)acetic acid 
• 1197374-06-3 montelukast 1-methyl-3-phenylpropyl amine salt 

Relevant academic research and scientific papers

Identification, synthesis and characterization of impurities of Montelukast sodium

Montelukast sodium is a selective leukotriene receptor antagonist which inhibits cysteinyl leukotriene CysLT1 receptor. Various synthesis of Montelukast is published. During laboratory optimization and later in bulk synthesis formation of various impurities was detected. Besides, pharma Europa draft mention nine process related impurities. However, the method of preparation of most of these impurities is not available in literature. Also, different route of synthesis will have different impurity profile and those process related impurities are not covered in pharmacopeias. In this study we report the synthesis of possible process impurities, including seven impurities (A-H) mentioned in pharma Europa.

AN IMPROVED PROCESS FOR PREPARING MONTELUKAST AND SALTS THEREOF

A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercapto methyl) cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.