Title of Invention | AN IMPROVED PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS AMINE SALTS |
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Abstract | The present invention provides an improved process for the preparation of [R- (E)-I- [[[I-[3-[2-[7-chloro-2-quinolinyl] ethenyl] phenyl]-3-[2-(I-hydroxy-I-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid (Montelukast) of Formula (1) and its amine salts comprising of primary, secondary and tertiary amines. The amine salts of Montelukast are precursor for the preparation of Montelukast sodium. The improved process for the preparation comprises, mesylation of 2-(2-(3(S)-(3-(2-(7-chloro-2- quinolinyl) ethenyl) phenyl)-3-hydroxypropyl) phenyl)-2-propanol of Formula (2) with methane sulfonyl chloride using triethyl amine as a base, the resulted mesylated compound of Formula (3) is condensed with I-(mercaptomethyl) cyclopropane aceticacid of Formula (4) in the presence of simple base such as sodium hydroxide and sodium methoxide in a solvent to afford the Montelukast. The Montelukast is further converted into its amine salts in a conventional methods. The process for the preparation of Montelukast and its amine salts of the present invention is simple, cost-effective and environment friendly. |
Full Text |
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505-mas-2002 correspondence others.pdf
505-mas-2002 correspondence po.pdf
505-mas-2002 description (complete).pdf
Patent Number | 236239 | ||||||||||||
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Indian Patent Application Number | 505/MAS/2002 | ||||||||||||
PG Journal Number | 42/2009 | ||||||||||||
Publication Date | 16-Oct-2009 | ||||||||||||
Grant Date | 12-Oct-2009 | ||||||||||||
Date of Filing | 05-Jul-2002 | ||||||||||||
Name of Patentee | DR REDDY'S LABORATORIES | ||||||||||||
Applicant Address | 7-1-27, ameerpet HYDERABAD-500016. | ||||||||||||
Inventors:
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PCT International Classification Number | C07D215/00 | ||||||||||||
PCT International Application Number | N/A | ||||||||||||
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PCT Conventions:
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