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US 2012/0259121 A1Published application
Process for the preparation of montelukast and salts thereof
AssigneePharmathen S.A.
InventorsTheoharis V. Koftis, Ravikant R. Soni
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Abstract
The present invention relates to an improved process for the preparation of Montelukast and pharmaceutical acceptable salts or derivatives thereof, in particular to a process for large scale production of Montelukast and salts thereof in high yield and high purity and pharmaceutical preparations containing said compounds.
Claims14
A process for the preparation of Montelukast sodium of Formula I, which comprises
- (a) dissolution of {S}-1-[3-[2-(7-chloro-2-quinolinyl)ethyl]phenyl]-3-[2-(1-hydroxyl-1-methylethyl)phenyl]propanol of Formula II in a solvent in the presence of catalyst and addition of mesyl chloride thereto to obtain a reaction mass;
- (b) addition of a solution of 2-[1-(mercaptomethyl)cyclopropyl]acetic acid of Formula III into the reaction mass obtained from step (a) followed by a solution of sodium methoxide and work-up to obtain crude Montelukast free acid of Formula IV;
- (c) reaction of crude Montelukast free acid of Formula IV with L-ephedrine to obtain crude Montelukast-L-ephedrine of Formula V;
- (d) purification of crude Montelukast L-ephedrine salt of Formula V in order to obtain substantial pure Montelukast-L-ephedrine of Formula V with chemical purity of not less than 99.5% and optical purity of not less than 99.9%;
- (e) conversion of the substantial pure Montelukast L-ephedrine salt of Formula V into substantial pure Montelukast sodium of Formula I.
2 more elements
Dependencies are inferred from the claim text.