- Preparation method of montelukast sodium drug intermediate
-
The invention relates to a preparation method of a montelukast sodium drug intermediate, wherein the method comprises the following steps: uniformly mixing a compound II, a compound III, alkali and a solvent, and carrying out chemical reaction at the temperature of 80-150 DEG C in the presence of a catalyst to prepare an intermediate compound I, wherein the catalyst is CuCl, CuBr or CuI; and specific synthetic route is described in the specification. According to the preparation method, the catalyst is low in cost, high in catalytic activity, mild in reaction condition and environmentally friendly, the yield reaches 90% or above, the purity reaches 99% or above, repeated cyclic utilization can be achieved after simple filtration and separation, and industrial production of the montelukast sodium drug intermediate is easier.
- -
-
Paragraph 0004; 0023-0037
(2021/05/01)
-
- For the synthesis of montelukast intermediate compound and its preparation method
-
The invention relates to a medicine intermediate and a preparation method thereof, and especially relates to an intermediate compound for synthesizing montelukast, and a preparation method thereof. The intermediate compound is represented by formula (2); and in the formula (2), R'' is a C1-4 alkyl group, and X is halogen.
- -
-
-
- Method for synthesizing montrlukast sodium intermediate by means of series catalysis of graphene palladium cobalt
-
The invention relates to a technology for chemical synthesis of a medicine intermediate, in particular to a method for synthesizing a montrlukast sodium intermediate-[S-(E)]-2-[3-[3-[2-(7-chlorine-2-quinolyl)vinyl]phenyl]-3-hydroxy propyl]methyl benzoate by means of series catalysis of graphene palladium cobalt. The method adopts two steps of coupling and reducing and a one-pot series catalytic system; the obtained intermediate product does not need to be separated; the method is simple in operation, high in yield and good in chiral selectivity, thus being suitable for industrial production.
- -
-
Paragraph 0007; 0013; 0014; 0015
(2017/08/30)
-
- Practical synthesis of methyl (E)-2-(3-(3-(2-(7-chloro-2-quinolinyl) ethenyl)phenyl)-3-oxopropyl)benzoate, a key intermediate of Montelukast
-
A novel and practical synthetic route is presented for the preparation of methyl-(E)-2-(3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-oxopropyl) benzoate, the key intermediate of Montelukast, a leukotriene antagonist. The main diarylpropane framework was prepared via a polarity conversation reaction resulting in an acyl anion equivalent followed by a nucleophilic substitution reaction. The overall yield of this approach was 61%. This method is simple for operation and suitable for industrial production.
- He, Liang,Guo, Yang Hui,Wang, Ya Ping,Wang, Xiang Jing,Zhang, Ji,Xiang, Wen Sheng
-
p. 518 - 520
(2012/06/16)
-
- 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; 6; 10; 11
(2010/06/20)
-
- PREPARATION OF MONTELUKAST AND ITS SALTS
-
There is provided a process for the preparation of montelukast of the Formula (I).
- -
-
Page/Page column 31-32
(2008/12/05)
-
- Process for the preparation of optically active ethenylphenyl-alcohols
-
Optically active ethenylphenyl-alcohols of formula or its mirror image, wherein R1 is unsubstituted or substituted heteroaryl and R2 is phenyl or substituted aryl, are prepared by asymmetric hydrogenation of the corresponding ketones applying hydrogen gas in the presence of specific platinum metal complex catalysts.
- -
-
Page/Page column 9
(2008/12/08)
-
- PROCESS FOR THE MANUFACTURE OF METHYL-2-(3-(2-(7-CHLORO-2-QUINOLINYL-ETHENYL)-PHENYL)-3-OXOPROPYL) BENZOATE
-
A process for the preparation of methyl 2-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-oxopropyl)benzoate of the formula II in high yield and purity.
- -
-
Page/Page column 5
(2008/06/13)
-
- A PROCESS FOR SYNTHESIZING DIOL (VIII)-AN INTERMEDIATE OF MONTELUKAST SODIUM
-
A process comprises preparing benzaldehyde of formula I in a conventional manner, reacting the said benzaldehyde I with Grignard reagent in water miscible etheral solvent to precipitate the alcohol of formula (II) by addition of ammonium salt and water followed by isolating the alcohol thus precipitated by any known methods and then oxidizing directly under "Swern's conditions" to get a ketone of formula m, enolizing the said ketone in presence of a mild base such as alkali metal alkoxide and then reacting it with dialkyl carbonate under conditions effective to yield a β- ketoester of formula IV, benzylating the said β-ketoester so obtained in the preceding step to form the benzoate of formula V in presence of mild inorganic base followed by decarboxylating the said benzoate to a mixture of a ketoester of formula VI and its corresponding acid of formula VIA in the presence of acidic conditions, alkylating the acid VIA present in the mixture in the preceding step to obtain ketoester of formula VI and purifying it if so desired, asymmetrically reducing the ketoester of formula VI, to a chiral alcohol of formula VII using (-) diisopinocamphenylchloroborane (-DIPC1) in presence of less than 4 times v/w aprotic solvent and optionally in presence of Lewis base with respect to the said ketoester of formula VI, treating the said chiral alcohol VII with cerium halo salt, and alkylmagnesium halide followed by isolating the title compound using hyflow supercel and ammonium chloride to get the intermediate diol of formula VIII. Atemately, the said alcohol to Heck coupling with methyl-2-iodobenzoate in presence of Lewis base, acetonitrile, and palladium acetate to yield ketoester (VI), which is converted to diol (VIII) as described herein above.
- -
-
Page/Page column 30-31
(2010/10/20)
-
- Practical route to a new class of LTD4 receptor antagonists
-
A general approach to the synthesis of a new class of LTD4 antagonists is presented. The key diarylpropane framework was prepared by Claisen-Schmidt condensation and selective reduction of the enone. Depending on the bridge to the 7-chloroquinaldine moiety, alkylation or Heck coupling methodology was developed. The chiral sulfides were introduced by asymmetric reduction of the diarylpropanone intermediates and subsequent inversion of the chiral center.
- Larsen, Robert D.,Corley, Edward G.,King, Anthony O.,Carroll, James D.,Davis, Paul,Verhoeven, Thomas R.,Reider, Paul J.,Labelle, Marc,Gauthier, Jacques Y.,Xiang, Yi Bin,Zamboni, Robert J.
-
p. 3398 - 3405
(2007/10/03)
-
- Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
-
Compounds having the formula I: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
- -
-
-
- QUINOLINE-CONTAINING KETOACIDS AS LEUKOTRIENE ANTAGONISTS
-
Compounds having the formula I: STR1 are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection.
- -
-
-
- Fluorinated hydroxyalkylquinoline acids as leukotriene antagonists
-
Compounds having the formula I: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
- -
-
-
- Diarylstrylquinoline diacids and pharmaceutical compositions thereof
-
Compounds having the formula: STR1 are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.
- -
-
-
