EventsThe 20th International Electronic Conference on Synthetic Organic Chemistry
Published
This submission belongs to the session b. Bioorganic, Medicinal and Natural Products Chemistry of the event The 20th International Electronic Conference on Synthetic Organic Chemistry
Published date
01 Nov, 2016
Citation
Javad Mokhtari Aliabad, Negin Hosseini, Issa Yavari, Morteza Rouhani, Development of an efficient and practical approach for the synthesis of intermediate of Montelukast Sodium, in Proceedings of The 20th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2016, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-20-b014
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Development of an efficient and practical approach for the synthesis of intermediate of Montelukast Sodium

Negin Hosseini 1
Issa Yavari 1
Morteza Rouhani 1
1. Department of Chemistry, Science and Research Branch, Islamic Azad University, Tehran, Iran
Abstract

Montelukast 1 is a famous drug demonstrated for the chronic and prophylaxis therapy of asthma. It behaves as a selective antagonist of the leukotriene D4 receptor which causes the decrease of broncho constriction and eventuates in less inflammation. Montelukast is prescribed orally once daily which gives a profit in contrast with other drugs for pulmonary diseases such as asthma. The low stability and complex synthesis of Montelukast 1 present multitude difficulties for its large-scale production. Our present study demonstrates a novel and the industrially scalable process for the preparation of sodium (S,E)-2-(1-(((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(methoxycarbonyl)phenyl)propyl)thio)methyl)cyclopropyl)acetate which is one of the key intermediates of the Montelukast sodium synthesis process. We demonstrated a novel process that resolves multitude prior limitations and problems. Our modified process (see in scheme 2), which details are shown in this paper, is appropriate for large-scale production of the active pharmaceutical ingredient (API) with many benefits generally known as Montelukast.

Keywords
Montelukast sodium
Singulair
asthma
drug synthesis
chronic therapy
Manuscript
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