cas 151767-02-1, Montelukast sodium | Articles data

Articles about 151767-02-1Total 81 be found

Article title
Article abstract
Author
Journal number and time
Download

Preparation method of montelukast sodium
The invention discloses a preparation method of montelukast sodium. The method comprises the following steps of: reacting a low-boiling-point organic amine salt of montelukast acid with alcohol serving as a solvent and an alcoholic solution of sodium hydroxide serving as alkali, performing concentrating under reduced pressure after the reaction is finished, adding water to dissolve to a specifiedconcentration, and conducting freeze-drying according to a corresponding freeze-drying procedure to obtain a montelukast sodium finished product meeting the requirements. The preparation method of montelukast sodium provided by the invention has the advantages of simple process, environmental protection, reduction of the use of a large amount of organic solvents, accordance with the characteristics of green chemistry and the like.
-
Paragraph 0092-0095

(2020/12/15)

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,
-
(2020/12/08)

Synthesis method of montelukast sodium
The invention belongs to the technical field of medicines, and particularly provides a montelukast sodium synthesis method, which comprises: (1) dissolving a compound represented by a formula (II) andan organic alkali in an organic solvent A under the protection of an inert gas, cooling, adding a tetrahydrofuran solution of a compound represented by a formula (III), and carrying out a stirring reaction to obtain a compound represented by a formula (IV); and (2) under the protection of inert gas, dissolving the compound represented by the formula (IV) in methanol, controlling the temperature,adding sodium hydroxide, adding a drying agent and activated carbon after the reaction is finished, stirring, filtering, concentrating under reduced pressure to obtain a compound crude product represented by a formula (I), and re-crystallizing the compound crude product represented by the formula (I) to obtain a compound refined product represented by the formula (I). According to the invention, the yield of the montelukast acid prepared according to the method is greater than 98%, the purity is higher than 99.7%, the yield of the prepared montelukast sodium is greater than 93.5%, and the purity is higher than 99.80%.
-
Paragraph 0020; 0050-0067

(2020/11/23)

A synthesis process of montelukast sodium (by machine translation)
A synthesis process of montelukast sodium, relates to the field of drug synthesis, adopts a double hydroxy precursor of a sulfonyl derivative, and mercapto carboxylic acid compound, b cyclohexylamine in the reaction under the action of a catalyst, to obtain the ammonium salt, the quaternary ammonium salt is converted into the montelukast sodium. Compared with the direct synthesis of montelukast sodium, synthetic ammonium salt reaction not only conversion is higher, but also easy to separate, high purity, thus being beneficial to obtain high-purity of montelukast sodium. The synthesizing process of the synthetic route is simple, easy to operate, low requirements on equipment, can realize the large-scale production of montelukast sodium. (by machine translation)
-
(2019/04/04)

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.
-
(2017/08/31)

METHOD FOR MANUFACTURING MONTELUKAST SODIUM
PROBLEM TO BE SOLVED: To provide a method for efficiently manufacturing high purity montelukast sodium without producing montelukast free acid. SOLUTION: There is provided a method of manufacturing high purity montelukast sodium by making a strong basic aqueous solution of sodium act on a montelukast amine salt represented by the following formula I, where R1 and R2 represent each independently hydrogen, an alkyl group or a cycloalkyl group, and R3 represents an alkyl group or a cycloalkyl group. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
-
Paragraph 0022

(2017/02/09)

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%.
-
Paragraph 0032

(2016/11/28)

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.
-
Paragraph 0035; 0049-0050

(2017/01/09)

Preparation method of montelukast sodium
The invention discloses a preparation method of montelukast sodium. The method comprises: A, converting a montelukast acid crude into a montelukast amino acid 2-amino-1-butanol salt; B, recrystallizing and refining the montelukast amino acid 2-amino-1-butanol salt; C, acidizing the montelukast amino acid 2-amino-1-butanol salt after refining, and freeing to obtain high-purity montelukast acid; and D, converting the montelukast acid into montelukast sodium. The preparation method of montelukast sodium has the advantages of simple process, high yield and good impurity removing effect, and the purity of the prepared montelukast sodium is more than 99.9%.
-
Paragraph 0037-0038; 0042-0048; 0052-0058

(2017/07/21)

Method for preparing montelukast acid
The invention discloses a method for preparing montelukast acid. The method comprises a reaction b or a reaction a to a reaction b in the following synthetic route: the formula is shown in the description. The method disclosed by the invention can be used for preparing montelukast acid and salts thereof with low cost and high yield by means of simple operations by using low-cost and easily available raw materials, and is of significance and has practical value to prepare montelukast acid and salts thereof with low cost on a large scale.
-
Paragraph 0045; 0046

(2016/10/08)

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
-
(2018/02/28)

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
-
Paragraph 0057; 0063

(2018/10/19)

METHOD OF MANUFACTURING AMORPHOUS OF SODIUM MONTELUKAST
PROBLEM TO BE SOLVED: To provide a method of efficiently manufacturing 1-(((1R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methyl ethyl)phenyl)propyl)thio)methyl)cyclopropane sodium acetate having reduced residual solvent content. SOLUTION: A solution which 1-(((1R)-(3-(2(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methyl ethyl)phenyl)propyl)thio)methyl)cyclopropane sodium acetate is solved in at least one kind selected from a group consisting of aromatic hydrocarbons and acetic acid esters is dropped in an aliphatic hydrocarbon having 5 to 8 carbon atoms at -10°C to 10°C to be immobilized. COPYRIGHT: (C)2015,JPOandINPIT
-
Paragraph 0050

(2016/12/22)

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.
-
Page/Page column 19

(2014/08/19)

PROCESS FOR PREPARATION OF MONTELUKAST SODIUM
Disclosed is a process for the preparation of montelukast sodium. The process comprises a) reacting 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxypropyl)phenyl)-2-propanol with methane sulfonyl chloride and coupling the resultant mesylate compound with l-(mercaptomethyl)cyclopropane acetic acid in presence of a base and free alkali source followed by saltification with an amine in a single step reaction and b) converting the montelukast amine salt to montelukast sodium salt.
-
(2014/01/17)

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.
-
(2013/07/25)

PROCESS FOR THE PREPARATION OF MONTELUKAST SODIUM
The present invention relates to a process for the synthesis of Montelukast sodium of formula I the chemical name of which is [(R)-(E)]-1-[[[1-[3-[2-(7-chloro-2- quinolinyl)ethenyl]phenyl] -3 - [2-( 1 -hydroxy- 1 -methylethyl)phenyl]propyl] thio]methyl] - -cyclopropaneacetic acid sodium salt. The present invention further provides compounds of general formulae V, VI, VIb and VIII as new intermediates.
-
(2012/03/09)

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.
-
(2012/02/13)

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.
-
(2012/10/18)

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.
-
(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.
-
(2012/06/30)

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.
-
(2012/10/07)

Purification of montelukast using simulated moving bed
This invention concerns generally with a process for purifying crude pharmaceutical compositions, wherein the crude pharmaceutical composition comprises a sodium salt of Montelukast and more particularly relates to a process for the production of pharmaceutically pure preparations of Montelukast sodium using simulated moving bed technology, without requiring an intermediate acid formation step to separate isomers and to remove impurities.
-
Page/Page column 9

(2012/06/16)

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.
-
Page/Page column 6

(2011/05/03)

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.
-
(2011/10/13)

PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS SALTS
-
-
(2011/04/14)

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.
-
(2011/07/09)

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.
-
Page/Page column 16

(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.
-
Page/Page column 12

(2011/04/14)

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.
-
Page/Page column 6

(2011/07/29)

METHOD FOR ISOLATION AND PURIFICATION OF MONTELUKAST
A method of isolation of Montelukast of formula I from reaction mixtures, comprising conversion of the crude sub-stance to well-crystallizing salts with primary amines in the environment of at least one organic solvent and acetonitrile, followed by re-crystallization of these salts with simultaneous removal of chemical impurities and use of the chemically pure salts of Montelukast with primary amines for direct transformation to the pharmaceutically useful amorphous form of Montelukast sodium of formula II.
-
Page/Page column 7

(2010/11/03)

Improved process for the preparation of montelukast: Development of an efficient synthesis, identification of critical impurities and degradants
An improved and scalable process for the production of montelukast (Singulair, drug for asthma) based on a new and advantageous method of carrying out the key substitution reaction has been developed. The present procedure is distinguished from the previous solutions in the use of linear or cyclic polyethers, which ensures higher selectivity of the key step. The improved process for the preparation of montelukast is able to minimize a content of impurities and allows the effective production of montelukast and its scale-up.
Halama, Ales,Jirman, Josef,Bouskova, Olga,Gibala, Petr,Jarrah, A. Kamal
experimental part
p. 425 - 431
(2011/04/22)

NOVEL INTERMEDIATES FOR PRODUCING [R-(E)]-1-[[[1-[3-[2-(7- CHLORO -QUINOLINYL)ETHENYL]PHENYL]-3-[2-(1-HYDROXY- METHYLETHYL) PHENYL]PROPYL]THIO] METHYL] CYCLOPROPANEACETIC ACID, MONOSODIUM SALT AND PROCESS THEREOF
Disclosed herein are novel intermediates for producing [R-(E)]-1-[[[1-[3-[2-(7- chloro-2-quinolinyl)ethenyl]phenyl] -3 - [2-(1-hydroxy- 1 -methylethyl) phenyl] propyl]thio] methyl] cyclopropaneacetic acid, monosodium salt (montelukast sodium). Further the invention provides processes for preparing said intermediates.
-
Page/Page column 9-10; 17

(2010/06/20)

PREPARATION OF MONTELUKAST
Processes for the preparation of montelukast and its salts.
-
Page/Page column 28-29

(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
-
Page/Page column 5; 8; 16; 17

(2010/06/20)

SPECIFIC IMPURITIES OF MONTELUKAST
The subject-matter of the invention consists in a method of removing specific impurities of montelukast of formula (I), which occur due to chemical instability of the target substance and also contaminate the substance in the preparation process. Further, methods of isolation of specific impurities of montelukast defined by formulae (V-A), (IV-A), (XIIIa-A), (XIIIb-A) and analytic methods used for the control of the production of montelukast in the pharmaceutical quality.
-
Page/Page column 21-22

(2009/10/22)

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.
-
Page/Page column 11-12

(2009/12/27)

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.
-
Page/Page column 23

(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)
-
Page/Page column 10

(2009/06/27)

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.
-
Page/Page column 14-15

(2009/05/28)

CRYSTALLINE SALT OF MONTELUKAST
Cyclopropylamine salt of montelukast in crystalline form and its use for the preparation of highly pure amorphous montelukast sodium.
-
Page/Page column 4

(2009/05/28)

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.
-
Page/Page column 8-9

(2009/07/17)

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).
-
Page/Page column 16

(2009/12/23)

PREPARATION OF MONTELUKAST AND ITS SALTS
Processes for preparing montelukast acid and its salts.
-
Page/Page column 24

(2009/10/22)

Process for the purification of montelukast
It relates to a process for the purification of Montelukast, or pharmaceutically salts thereof, or solvates thereof, including stereoisomers or mixture thereof which comprises carrying out a specific set of selective solvent extractions of Montelukast or its impurities in a mixture of an organic solvent and water at specific ranges of pH and temperature which depend on the type of impurities to remove. In particular, it comprises at least one wash of an aqueous phase containing crude Montelukast in salt form with an organic solvent, at a pH comprised between 12.0 and 13.5; and optionally one or more washes of the resulting aqueous phase with an organic solvent at a pH comprised between 8.5 and 10.0. Montelukast is recovered by acidification at a pH comprised between 4.5 and 8.0 and solvent extraction, and is isolated either as acid or in salt form.
-
Page/Page column 8

(2008/06/13)

Purification process of montelukast and its amine salts
It comprises a process for the purification of Montelukast, or its salts or its solvates, including any stereoisomer or mixture thereof, which comprises converting Montelukast acid or a solvate thereof, including any stereoisomer or mixtures thereof, into an amine salt selected from the group consisting of cyclohexylamine, tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, R-(+)-α-methylbenzylamine, and L-(+)-α-phenylglycinol salt, in the presence of an appropriate solvent. It also comprises novel salts of Montelukast, in particular, cyclohexylamine, tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, R-(+)-α-methylbenzylamine, and L-(+)-α-phenylglycinol salts.
-
Page/Page column 10

(2008/06/13)

PREPARATION OF MONTELUKAST AND ITS SALTS
There is provided a process for the preparation of montelukast of the Formula (I).
-
Page/Page column 43

(2008/12/05)

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.
-
Page/Page column 14

(2008/06/13)