Montelukast and Its Impurities

Leukotrienes are inflammatory mediaters that are produced by the immune system and serve to promote bronchoconstriction, inflammation, microvascular permeability, and mucus secretion in asthma and COPD.

Numerous leukotriene receptor antagonists are used to treat these diseases, and one such drug which is developed by Merck is Montelukast.

Montelukast is used regularly to prevent wheezing and shortness of breath during asthma and also helps in decreasing the number of asthma attacks. It is also helpful in treating hay fever and allergic rhinitis.

Montelukast is synthesized synthetically and several process related impurities, metabolites, intermediates, degradation products are associated with the product and 27 of such impurities are successfully identified and synthesized at one of the leading CRO in India, Pharmaffiliates Analytics and Synthetics P. Ltd.

The impurities which are available at Pharmaffiliates are named and classified as following:-

·       Montelukast impurity A (S-isomer of Montelukast), B (impurity in commercial synthesis), C (metabolite M2 of Montelukast), D and E ( impurity and part of diastereomeric mixture), F ( a ketone impurity), G (a cis isomer present as impurity), I (hydroxylated impurity)

·       Montelukast Sodium (sodium salt of Montelukast)

·       1-{3-[2-(7-Chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propan-1-ol (impurity in commercial synthesis)

·       1-(Mercaptomethyl)cyclopropane acetic acid (intermediate formed in synthesis of Montelukast)

·       Montelukast (3S)-hydroxy benzoate (intermediate formed in synthesis of Montelukast)

·        Methyl 2-(3-{3-[2-(7-chloroquinolin-2-yl)vinyl]phenyl}-3-oxopropyl)benzoate  (impurity formed in commercial synthesis)

·       Montelukast 1,2-diol (methyl-hydroxyl metabolite, exists as mixture of diastereomers)

·        Montelukast sulfone (impurity formed in commercial synthesis)

·       Montelukast disulfide impurity (impurity formed in commercial synthesis)

·       Montelukast ether impurity (cyclised ether impurity)

·       Montelukast dicyclohexylamine (dicyclohexylamine salt)

·       Montelukast dihydro impurity (impurity formed in commercial synthesis)

·       Montelukast lactone (impurity formed in commercial synthesis)

·       Montelukast amide (impurity formed in commercial synthesis)

·       Montelukast cyclopropane acetonitrile (impurity formed in commercial synthesis)

·       Montelukast (3S)-hydroxy propanol (impurity formed in commercial synthesis)

·       Montelukast 3-oxo propanol (impurity formed in commercial synthesis)

·       7-Chloroquinaldine (intermediate formed in synthesis of Montelukast)

·       2-[3-(R)-[3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl]-3-hydroxypropyl]phenyl-2-propanol (intermediate formed in synthesis of Montelukast)

·       Mixture of Montelukast sodium, and Montelukast methyl impurity 

 

All the impurities supplied by Pharmaffiliates are with complete structure elucidation and data interpretation with high end analytical techniques like NMR, MASS and Chromatographic purity along with detailed Certificate of Analysis.

All the above mentioned products are available at Pharmaffilites Analytics and Synthetics at very competitive prices. Pack sizes of 25mg, 50mg or customized packs as per the need of the customer are also available with us.