807638-71-7

Upstream product

• 287930-77-2 (S,E)-1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propan-1-ol 
• 7143-01-3 Methanesulfonic anhydride 
• 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 
• 124-63-0 methanesulfonyl chloride 

Downstream Products

• 158966-92-8 montelukast 
• 851755-58-3 montelukast tert-butylamine salt 
• 577953-88-9 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt 
• 866923-62-8 2-(1-((((R)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propyl)sulfanyl)methyl)cyclopropyl)acetonitrile 
• 168214-68-4 2-[2-((E)-3-{3-[(E)-2-(7-Chloro-quinolin-2-yl)-vinyl]-phenyl}-allyl)-phenyl]-propan-2-ol 
• 880769-26-6 1-(((1-(R)-(3-(2-(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl) thio)methyl)cyclopropaneacetic acid dipropylamine salt 
• 151767-02-1 Montelukast sodium 
• 1197374-06-3 montelukast 1-methyl-3-phenylpropyl amine salt 
• 1380816-64-7 montelukast 1-(1-naphthyl)ethylamine salt 
• 1187586-61-3 [R, E]-[[1-[3-[2-(7-chloro-2-quinolinyl)-2-(S)-[(carboxymethyl)cyclopropyl]methyl]thio]ethyl]phenyl]-3-[[[[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropane acetic acid 
• 1187586-58-8 [R, E]-[[1-[3-[2-(7-chloro-2-quinolinyl)-2-(R)-[(carboxymethyl)cyclopropyl]methyl]thio]ethyl]phenyl]-3-[[[[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropane acetic acid 
• 168214-67-3 C₂₉H₂₆ClNO 
• 909849-96-3 [R,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]-phenyl]-3-[2-(-hydroxy-1-methylethyl) phenyl]propyl]-sulfinyl] methyl] cyclopropaneacetic acid 
• 1187364-41-5 [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid homoveratrylamine salt 

Relevant academic research and scientific papers

A synthesis process of montelukast sodium (by machine translation)

A synthesis process of montelukast sodium, relates to the field of drug synthesis, adopts a double hydroxy precursor of a sulfonyl derivative, and mercapto carboxylic acid compound, b cyclohexylamine in the reaction under the action of a catalyst, to obtain the ammonium salt, the quaternary ammonium salt is converted into the montelukast sodium. Compared with the direct synthesis of montelukast sodium, synthetic ammonium salt reaction not only conversion is higher, but also easy to separate, high purity, thus being beneficial to obtain high-purity of montelukast sodium. The synthesizing process of the synthetic route is simple, easy to operate, low requirements on equipment, can realize the large-scale production of montelukast sodium. (by machine translation)

Menglusitena a high yield new method for the synthesis of (by machine translation)

The invention discloses a method for preparing Menglusitena, the method adopts a one-pot synthesis, in order to 2 - (2 - (3 - (2 - (7-chloro-2-quinolyl) vinyl) phenyl) - 3-oxo-propyl) phenyl) propyl alcohol as the starting material, and 1 - (thiomethyl)-c

METHOD FOR PRODUCING MONTELUKAST ALKYL ESTER

PROBLEM TO BE SOLVED: To provide a method for efficiently producing a high purity 1-(((1(R)-(3-(2-(7-chloro-2-quinonyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid alkyl ester having a reduced content of a specific impurity. SOLUTION: A specific amount of a weakly basic nitrogen-containing organic compound is made to exist in a reaction system in a reaction between 2(2-(3(S)-(3-(2-(7-chloro-2-quinonyl)ethenyl)phenyl)-3-methanesulfonyloxypropyl)phenyl)-2-propanol and 1-mercaptomethylcyclopropane acetic acid alkyl ester in the presence of a strong base. COPYRIGHT: (C)2015,JPO&INPIT

PROCESS FOR PREPARATION OF MONTELUKAST SODIUM

Disclosed is a process for the preparation of montelukast sodium. The process comprises a) reacting 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxypropyl)phenyl)-2-propanol with methane sulfonyl chloride and coupling the resultant mesylate compound with l-(mercaptomethyl)cyclopropane acetic acid in presence of a base and free alkali source followed by saltification with an amine in a single step reaction and b) converting the montelukast amine salt to montelukast sodium salt.

PROCESSES FOR PREPARATION OF MONTELUKAST SODIUM AND PURIFICATION OF DIOL INTERMEDIATE

A process for preparation of montelukast sodium through novel montelukast amine salts is provided, wherein the amine is selected from 1- (l-naphthyl)ethylamine, S-methyl-L-cysteine, diallylamine or isomers thereof. A process for purification of 2-(2-(3-(S)-(3-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxylpropyl)-phenyl-2-propanol is also provided, which uses a halogenated hydrocarbon and a nitrile as solvent.

MONTELUKAST HEXAMETHYLENEDIAMINE SALT AND ITS USE FOR THE PREPARATION OF MONTELUKAST SODIUM

The present invention relates to a montelukast hexamethylenediamine, Formule (I). It also relates to a process for the preparation of montelukast hexamethylenediamine and its use for the preparation of Montelukast Sodium.

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.

Improved process for the preparation of montelukast: Development of an efficient synthesis, identification of critical impurities and degradants

An improved and scalable process for the production of montelukast (Singulair, drug for asthma) based on a new and advantageous method of carrying out the key substitution reaction has been developed. The present procedure is distinguished from the previous solutions in the use of linear or cyclic polyethers, which ensures higher selectivity of the key step. The improved process for the preparation of montelukast is able to minimize a content of impurities and allows the effective production of montelukast and its scale-up.

NOVEL INTERMEDIATES FOR PRODUCING [R-(E)]-1-[[[1-[3-[2-(7- CHLORO -QUINOLINYL)ETHENYL]PHENYL]-3-[2-(1-HYDROXY- METHYLETHYL) PHENYL]PROPYL]THIO] METHYL] CYCLOPROPANEACETIC ACID, MONOSODIUM SALT AND PROCESS THEREOF

Disclosed herein are novel intermediates for producing [R-(E)]-1-[[[1-[3-[2-(7- chloro-2-quinolinyl)ethenyl]phenyl] -3 - [2-(1-hydroxy- 1 -methylethyl) phenyl] propyl]thio] methyl] cyclopropaneacetic acid, monosodium salt (montelukast sodium). Further the invention provides processes for preparing said intermediates.

AN IMPROVED PROCESS FOR THE PREPARATION OF MONTELUKAST SODIUM AND ITS INTERMEDIATES

The present invention relates to a process for the preparation of montelukast sodium (formula 1) and formula 4. The invention concerns the coupling of thiol derivative, Methyl 1 - (mercaptomethyl)cyclopropane acetate with mesylate of formula 4 compound using alkyl substituted ammonium hydroxide base, alkali amides and purification of Montelukast acid by crystallization in suitable organic solvents. The invention further concerns to provide an improved process of montelukast intermediates having good yield and quality