cas 158966-92-8, Montelukast | Articles data

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Montelukast sodium intermediate compound
The invention provides a novel montelukast sodium intermediate compound and a preparation method thereof. The intermediate compound is good in stability and convenient to store; the intermediate compound serves as a starting material of montelukast sodium, the synthesized montelukast sodium is high in yield and good in purity; and the structural formula of the intermediate compound is shown in thespecification,
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Paragraph 0066; 0067

(2020/12/08)

Montelukast sodium intermediate and preparation method and application thereof
The invention relates to a series of novel compounds as shown in a formula (III) and a preparation method thereof. The invention also relates to an application of the novel compounds as shown in the formula (III) in synthesizing Montelukast sodium. The compounds as shown in the formula (III) are critical intermediates in the Montelukast sodium synthesizing process, and play a critical role of synthesizing the final target compound. The intermediate is stable in chemical property, the preparation process is mild in reaction condition, the yield is high, the optical purity is high, and the intermediate is suitable for large-scaled production. The formula is as shown in the description.
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Paragraph 0101; 0102; 0103

(2017/08/31)

Production of montelukast
PROBLEM TO BE SOLVED: To provide a method of producing a montelukast with raw materials which are easy to handle and inexpensive and in simple reaction operations.SOLUTION: A method of producing a montelukast includes mixing a 1-(mercaptomethyl)cyclopropane acetic acid and an alcohol solution of a sodium methoxide and/or a sodium ethoxide in an aromatic hydrocarbon solvent, adding a reaction accelerator and then adding 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(methanesulfonyloxypropyl)phenyl)-2-propanol to the resultant disodium dianion solution to react them.
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Paragraph 0009; 0019; 0023

(2017/08/02)

The crystal manufacturing method [...]
PROBLEM TO BE SOLVED: To provide a method for efficiently manufacturing dipropylamine 1-(((1(R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methylcyclopropaneacetate by reacting dipropylamine with a crude form of 1-(((1(R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methylcyclopropaneacetic acid.SOLUTION: When synthesizing dipropylamine 1-(((1(R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methylcyclopropaneacetate, a solvent mixture of butyl acetate and a hydrocarbon having 5-7 carbon atoms is used as a solvent, and crystals are deposited from a solution.
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Paragraph 0056

(2017/12/27)

And Menlust sodium process for the preparation of intermediates
The invention relates to a method suitable for preparing montelukast sodium and intermediate 2-(3(S)-(3-(2-(7-chlorine-2-quinolyl) vinyl) phenyl)-3-hydroxypropyl) phenyl)-2-propoxy) tetrahydropyrane (intermediate 3) of the montelukast sodium in a large scale. According to the method, 7-chloroquinaldine and 3-cyanobenzaldehyde are used as starting raw materials, 2-(3-(3-(2-(7-chlorine-2-quinolyl) vinyl) phenyl)-3-oxopropyl) phenyl)-2-propoxy) tetrahydropyrane (intermediate 2) is obtained by six steps of reaction, then intermediate 3 with ee more than 99% and yield more than 90% is obtained by chiral reduction, and the montelukast sodium with high optical purity and high chemical purity is obtained by the intermediate 3 through four steps of reaction.
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Paragraph 0032; 0047-0048

(2017/01/09)

Preparation method of montelukast
The invention discloses a preparation method of montelukast. An inorganic base solution is cooled to 0-10 DEG C, 1-(mercaptomethyl)-cyclopropaneacetic acid is added, and a stirred reaction is performed to obtain a 1-(mercaptomethyl)-cyclopropaneacetic acid dianion base solution; a quinolinediol compound is dissolved into water, and inorganic base and a phase transfer catalyst are added for stirring and even mixing; after the mixture is cooled to 0-10 DEG C, paratoluensulfonyl chloride is added for a reaction to obtain a tosylate compound solution, and then the tosylate compound solution is added into the 1-(mercaptomethyl)-cyclopropaneacetic acid dianion base solution for a stirred reaction to obtain a water solution of montelukast; then the montelukast solid is obtained through post-treatment. The method is simple in technology, mild in reaction condition, economical, environmentally friendly and high in yield and makes industrialized production easy.
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Paragraph 0037; 0038; 0039; 0040

(2017/01/02)

Method for preparing montelukast sodium from montelukast acid
The invention discloses a preparation method of montelukast sodium. The preparation method comprises: converting a montelukast acid crude product into a montelukast acid p-amino acetanilide salt, specifically, dissolving the montelukast acid crude product in an acetone/n-hexane mixture, adding p-amino acetanilide, stirring for reaction for 7-10 hours at 15-30 DEG C, then adding cyclohexane which accounts for 1/4 of the total volume of the acetone/cyclohexane mixture, stirring for reaction for 2 hours at 20 DEG C, and carrying out filtration and drying to obtain the montelukast acid p-amino acetanilide salt, wherein the mole ratio of montelukast acid to p-amino acetanilide is 1:1.5-2.0; recrystallizing to refine the amine salt; acidifying the refined amine salt, and carrying out dissociation to obtain high-purity montelukast acid; and converting the montelukast acid into montelukast sodium. The preparation method of montelukast sodium disclosed by the invention is simple in process, high in yield and good in impurity removal effect, the purity of the prepared montelukast sodium is more than 99.9%, and the content of styrene and sulfoxide impurities is lower than 0.02%.
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Paragraph 0031

(2016/11/28)

Asymmetric Catalysis with Iron-Salen Complexes
Iron(III)-salen complexes based on a chiral cis-2,5-diaminobicyclo[2.2.2]octane scaffold are used as catalysts for a variety of stereo selective reactions. High enantio- and diastereoselectivities can be achieved with these catalysts in sulfa-Michael conjugate addition to acyclic α,β-unsaturated ketones, in regioselective δ-addition of thiols to acyclic α,β,γ,δ-unsaturated ketones, and in Conia-ene carbocyclization of alkynyl-substituted β-dicarbonyl compounds. The use of these chiral iron-salen complexes as catalysts provides a new method for conducting these three important reactions under environmentally sustainable conditions.
Shaw, Subrata,White, James D.
p. 2768 - 2780
(2016/08/31)

Preparation method of montelukast sodium intermediates
The invention relates to a preparation method of montelukast sodium intermediates. The method comprises the steps that under the protection of inert gas, in solvent, nucleophilic substitution is conducted on a montelukast mother nucleus compound, replaced by various leaving groups, of secondary hydroxyl and various side chains respectively under the action of a catalyst, and various montelukast sodium intermediates are obtained. According to the preparation method of the montelukast sodium intermediates, new catalysts of 4-dimethylaminopyridine and 4-pyrrolidinopyridine are utilized, the reaction is mild in condition and rapid, the product is single, purification is easy and convenient, the obtained intermediates are high in optical purity and higher in yield, and the preparation method is more suitable for industrial production.
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Paragraph 0031; 0032; 0033

(2016/12/26)

METHOD FOR PRODUCING CRYSTAL OF MONTELUKAST FREE ACID
PROBLEM TO BE SOLVED: To provide a method for producing high-purity 1-(((1(R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid (montelukast free acid) efficiently in high yield. SOLUTION: The method for producing high-purity montelukast free acid, in which acid salt of organic amine salt does not remain, efficiently in high yield comprises a step of continuously performing such a reaction that montelukast organic amine salt is led to the montelukast free acid by using an acid in a mixture of a water-soluble organic solvent with water and continuously crystallizing the montelukast free acid from the obtained reaction solution. COPYRIGHT: (C)2015,JPO&INPIT
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Paragraph 0057; 0058; 0060-0062; 0064; 0065

(2018/10/19)

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
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(2018/02/28)

Iron catalyzed enantioselective sulfa-Michael addition: A four-step synthesis of the anti-asthma agent Montelukast
A salen ligand based on a chiral cis-2,5-diaminobicyclo[2.2.2]octane scaffold forms an iron(iii) complex with ferric chloride which catalyzes asymmetric addition of thiols to α,β-unsaturated ketones under mild conditions. The reaction (sulfa-Michael addition) produces β-thioketones in excellent yield and high enantiomeric excess from a wide range of aliphatic and aromatic thiols using chalcones and other conjugated enones as Michael acceptors. With α-substituted α,β-unsaturated ketones as acceptors, the addition shows strong preference (typically >50:1) for the syn diastereomer over the anti product. An asymmetric synthesis of (R)-Montelukast, the sodium salt of which is the commercial anti-asthma drug Singulair, was devised using conjugate addition of a thiol catalyzed by our iron(iii)-salen complex to an α,β-unsaturated ketone synthesized in a four-component, one-pot tandem Michael-aldol condensation. The reaction sequence to (R)-Montelukast proceeded in 72% overall yield over four steps from commercially available materials. A mechanism for our catalyzed asymmetric sulfa-Michael addition is advanced which coordinates the enone acceptor to the metal centre of the iron-salen complex in an open lower quadrant under the bicyclic scaffold, thereby exposing only the si face of the double bond to attack by the external nucleophilic thiol. Prior internal coordination of the thiol to the metal centre of the complex is proposed based on spectroscopic and chemical evidence and leads to activation of the catalyst through a trans ligand effect. This journal is the Partner Organisations 2014.
White, James D.,Shaw, Subrata
p. 2200 - 2204
(2014/05/20)

AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM
The present invention disclosed herein is a cost effective, in-situ process for the preparation of montelukast or its pharmaceutically acceptable salts of formula (1) by reacting optically pure (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methyl ethyl) phenyl]-propan-I-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by insitu condensing the same with disodium salt of mercapto-cyclopropyl acetic acid of formula (3) to afford montelukast free acid in good yield and purity, then converting the montelukast free acid into its substituted amine salt of formula (4). Further the montelukast substituted amine is converted into its pharmaceutically acceptable salt.
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(2014/08/19)

New and practical synthesis of montelukast sodium, an antiasthmatic drug
A new and practical synthesis of montelukast sodium, an antiasthmatic drug, is described. The key steps are the synthesis of nitrile derivative 4 by chiral reduction of keto ester 9 using (-)-DIP-Cl, synthesis of vinylquinoline framework 16 by Wittig reaction, and Heck coupling of nitrile 4 with vinylquinoline 16. The method is operationally simple and suitable for the industrial production of the drug substance. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file.
Saravanan,Satyanarayana,Reddy, P. Pratap
p. 2050 - 2056
(2013/06/27)

NOVEL MONTELUKAST 4-HALOBENZYLAMINE SALT AND METHOD FOR PREPARING MONTELUKAST SODIUM SALT BY USING THE SAME
Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. In Formula 2, X represents F, Cl, Br or I.
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Paragraph 0059; 0060; 0061; 0062; 0063

(2013/07/25)

MONTELUKAST INTERMEDIATE CAMPHORSULFONIC SALT
The present invention is directed to a novel salt of a montelukast intermediate, the process of preparation thereof, the use of such salt in the preparation of sodium montelukast and a process for the preparation of sodium montelukast making use of said salt.
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(2012/10/07)

Camphorsulfonic salt of a key Montelukast intermediate
The present invention is directed to a novel salt of a montelukast intermediate, the process of preparation thereof, and use of such salt in the preparation of sodium montelukast via a new amine salt of montelukast.
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(2012/10/18)

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.
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Page/Page column 27

(2012/06/30)

NOVEL MONTELUKAST 4-HALOBENZYLAMINE SALT AND METHOD FOR PREPARING MONTELUKAST SODIUM SALT BY USING THE SAME
Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. (Formular I and II should be inserted here) In Formula 2, X represents F, CI, Br or I.
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Page/Page column 11-12

(2012/02/13)

PROCESS FOR THE PREPARATION OF MONTELUKAST AND SALTS THEREOF
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.
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Page/Page column 5

(2012/10/18)

PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS SALTS THEREOF
The present invention relates to the alkyl amine salts of Montelukast and methods for their preparation and conversion of Montelukast amine salts to Montelukast or Montelukast alkali/alkaline salt.
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Page/Page column 6

(2011/05/03)

PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS SALTS
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Page/Page column 9

(2011/04/14)

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.
Sunil Kumar,Anjaneyulu,Hima Bindu
p. 4536 - 4546
(2012/02/04)

EFFICIENT SYNTHESIS FOR THE PREPARATION OF MONTELUKAST AND NOVEL CRYSTALLINE FORM OF INTERMEDIATES THEREIN
The present invention describes the improved process for the preparation of montelukast acid (VII) and its pharmaceutically acceptable salts and esters using a novel synthesis step. The process is cost effective, environment friendly, and easily scale up to commercial level and leads to products having high chemical and optical purity. Moreover, the present invention provides a novel crystalline intermediate (IV) that is useful in this process and a method for its production. In a further aspect, the process of the present invention includes a step of removing ketone by-products be derivatization.
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(2011/10/13)

METHOD FOR PREPARING MONTELUKAST SODIUM SALTS
Disclosed is a method for preparing a montelukast sodium salt of Formula 1. The method includes coupling a methanesulfonyl compound of Formula 2 below with a compound of Formula 3 below in the presence of a bistrimethylsilylamide alkali metal salt, further adding an alkali metal base thereto and hydrolyzing the mixture by heating to prepare a compound of Formula 4 below, reacting the compound of Formula 4 with 4-tert-butylcyclohexylamine, followed by purification, to prepare an amine salt of Formula 5, and converting the amine salt of Formula 5 into a sodium salt.
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Page/Page column 5

(2011/07/29)

IMPROVED PROCESS FOR THE PREPARATION OF MONTELUKAST AND SALTS THEREOF
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.
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Page/Page column 6

(2011/07/09)

METHOD FOR PREPARATION OF MONTELUKAST ACID IN IONIC LIQUID MEDIUM
The present invention relates to a method for preparing Montelukast acid or its sodium salt by reacting a thiol compound with a Montelukast intermediate in the presence of a base in a medium comprising an ionic liquid compound. In accordance with the inventive method, highly pure Montelukast acid or its sodium salt, which is advantageously used as a raw material in the preparation of Montelukast, a leukotriene antagonist, can be easily prepared in a high yield.
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(2011/05/08)

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.
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(2011/02/24)

Efficient synthesis for the preparation of montelukast
The present invention describes the improved process for the preparation of montelukast acid and its pharmaceutically acceptable salts and esters. The process is cost effective, environment friendly, and easily scale up to commercial level.
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Page/Page column 10

(2011/04/14)

PREPARATION OF MONTELUKAST
Processes for the preparation of montelukast and its salts.
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Page/Page column 26

(2010/12/31)

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
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Page/Page column 5; 8; 15; 16

(2010/06/20)

AN IMPROVED PROCESS FOR PREPARING MONTELUKAST AND SALTS THEREOF
A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercapto methyl) cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.
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Page/Page column 10

(2009/12/27)

A PROCESS FOR PREPARATION OF MONTELUKAST SODIUM SALT
The present invention relates to a process for the preparation of montelukast sodium salt. The process includes (a) reacting 2-(2-(3-(S)-(3-(7-chloro-2- quinolinyl)-ethenyl) phenyl)-3-hydroxypropyl)- phenyl-2-propanol of Formula (II) with diphenyl chloro phosphate to get a compound of Formula III; (b) condensing the compound of Formula III with a compound of Formula IV to get compound of Formula V; (c) and converting the compound of Formula V to montelukast sodium of Formula (I).
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Page/Page column 14-15

(2009/12/23)

MONTELUKAST BENZHYDRYL PIPERAZINE SALTS AND PROCESS FOR PREPARATION THEREOF
The invention relates to Benzhydryl piperazine salts of [R-(E)] -1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl]-3-[2-(1 -hydroxy-1-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid represented by the formula (III). Furthermore, the invention relates to the use of Benzhydryl piperazine salts of [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid represented by the formula (III) for the preparation of substantially pure [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]phenyl] -3 -[2-(1-hydroxy-1- methylethyl) phenyl] propyl] thio] methyl] cyclopropane acetic acid or its alkali, salts and pharmaceutical composition comprising the same.
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Page/Page column 19-20

(2009/10/22)

PROCESS FOR THE PURIFICATION OF MONTELUKAST BY THE PREPARATION OF ACID ADDITION SALTS AND TERT-AMYLAMINE SALT
The present invention relates to processes for the purification of montelukast by the preparation of acid addition salts and tert-amylamine salt. The preparation of acid addition salts is very efficient and does not lead to the increase of impurities arising from the dehydration of the tertiary alcohol, such as styrene impurity, while the use of tert-amylamine salt highly reduces the content of styrene impurity and montelukast sulfoxide.
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Page/Page column 12

(2009/10/09)

PREPARATION OF MONTELUKAST AND ITS SALTS
Processes for preparing montelukast acid and its salts.
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Page/Page column 13

(2009/10/22)

Process for the Preparation of Montelukast and its Salts
The present invention relates to an improved process for the preparation of 1-[[[(1R)-1-[3[(1E)-2-(7chloro-2-quinolinyl) ethenyl] phenyl]-3-[2-(1-hydroxy-1-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid (Formula-1) and its salts using Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl) ethenyl] phenyl]-3-halopropyl] benzoate (Formula-2)
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Page/Page column 9

(2009/06/27)

SALTS OF MONTELUKAST AND PROCESS THEREFOR
The present invention relates to new salts (II) of Montelukast (I) and process for preparing these salts where B is ammonia, benzylamine or phenyl hydrazine. The invention also provides a process for preparation amine salts comprising (a) dissolving/ suspending the Montelukast free acid of formula (I) in an organic solvent (b) reacting with an amine (c) isolating the amine salt of formula (II) by adding optionally another anti-solvent, and (d) optionally drying the isolated solid under vacuum. The invention provides a process for preparation of sodium salt of montelukast acid comprising lowering pH of aqueous solution of amine salt of montelukast having formula II to 5.0±0.5, raising pH to above 8.0 using source of sodium ion, and isolating, the sodium salt by crystallization.
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Page/Page column 8

(2009/04/25)

Process for the Preparation of Montelukast and Its Pharmaceutically Acceptable Salts
An improved process for the preparation of Montelukast and its pharmaceutically acceptable salts comprises of reacting (S) Benzenepropanol α-[3-[2-(7-chloro2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy-1-methyl ethyl)-α-methane sulfonate compound of formula (II) with 1-(mercapto methyl)cyclo propane acetic acid or its ester or nitrile in presence of alkali or alkaline carbonates and/or alkali or alkaline earth metal alkoxide in a suitable polar aprotic solvent with or without combination of C1-C4 alcoholic solvents and then treating with organic amine in a suitable ester and/or acetone and/or aliphatic or aromatic hydrocarbon solvents, and converting the corresponding amine salt compound of montelukast into its sodium salt compound of formula (I) using sodium ion source in methanol, without converting into montelukast free acid.
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Page/Page column 7-8

(2009/07/17)

CRYSTALLINE SALT OF MONTELUKAST
Cyclopropylamine salt of montelukast in crystalline form and its use for the preparation of highly pure amorphous montelukast sodium.
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Page/Page column 3

(2009/05/28)

CRYSTALLINE SALT OF MONTELUKAST
The present invention refers to the novel cyclopropylamine salt of montelukast in crystalline form and its use in the process for the preparation of highly pure amorphous montelukast sodium.
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Page/Page column 10-11

(2009/05/28)

Process for the Preparation of Leukotriene Receptor Antagonist (Montelukast Sodium)
The present invention relates to an improved process for the preparation of [R-(E)]-1-[[[1-[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropaneacetic acid, monosodium salt of Formula (I).
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Page/Page column 7

(2010/01/31)

PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS SALTS THEREOF
The present invention relates to the alkyl amine salts of Montelukast and methods for their preparation and conversion of Montelukast amine salts to Montelukast or Montelukast alkali/alkaline salt.
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Page/Page column 14

(2008/06/13)

PROCESS FOR THE PREPARATION OF MONTELUKAST, AND INTERMEDIATES THEREFOR
The invention relates to processes for making montelukast and to intermediates for use in the process, in particular compounds of formulas 2-7: L=OAc, OTs, OTf5OMs; where X=Cl, Br, I.
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Page/Page column 27

(2008/06/13)

PROCESS
A process of preparing montelukast, or a pharmaceutically acceptable salt thereof, which process comprises reacting a protected intermediate of formula (II) as defined in the specification with a cyclopropyl intermediate.
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Page/Page column 29-30

(2008/06/13)

Novel Compounds and Preparation for Montelukast Sodium
This invention relates to novel compounds and a process for preparation of montelukast sodium.
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Page/Page column 4-5

(2008/06/13)

METHOD OF PREPARING MONTELUKAST AND INTERMEDIATES USED THEREIN
The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.
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Page/Page column 9

(2008/12/06)

PREPARATION OF MONTELUKAST AND ITS SALTS
There is provided a process for the preparation of montelukast of the Formula (I).
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Page/Page column 40-41

(2008/12/05)

PROCESS FOR PREPARING MONTELUKAST AND SALTS THEREOF USING OPTICALLY IMPURE 2-(2-(3(S)-(3-(7-CHLORO-2-QUINOLINYL)ETHENYL)PHENYL)-3-HYDROXYPROPYL)PHENYL-2-PROPANOL
A process for preparing montelukast and salts thereof using an optically impure 2-(2-(3(S)-(3-(7-chloro-2-quinolinyl)-ethenyl)-phenyl)-3-(hydroxylpropyl)phenyl)-2 propanol as starting material, which contains the (R)-enantiomer impurity in the range of greater than 0.5% to about 8.0% by weight, is disclosed. The process described herein using an optically impure material results in the final product, montelukast sodium, in optical purity of greater than 99.7% enantiomeric excess.
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Page/Page column 12-13

(2008/12/08)

A NEW PROCESS FOR THE PREPARATION OF MONTELUKAST
The present invention describes a novel process for the preparation of montelukast acid, and its pharmaceutically acceptable salts and esters.
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Page/Page column 34

(2008/12/05)