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151767-02-1

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151767-02-1 Usage

Pharmacological effect

Cysteinyl leukotrienes (LTC4, LTD4, LTE4) is a eicosane-type substance released by various kinds of cells including mast cells and eosinophils with strong inflammatory effect. These important asthma pre-inflammatory mediators can bind to the Cysteinyl leukotriene receptors (CysLT) identified in the human airways, resulting in a variety of airway responses including bronchoconstriction, mucus secretion, increased vascular permeability, and eosinophil accumulation. Montelukast sodium is an orally active selective leukotriene receptor antagonist that can specifically inhibit the cysteinyl leukotriene receptor. It was successfully developed by the Merck Company (German) and had entered into market in Canada, Finland, and Mexican in 1997. It is suitable for the prevention and long-term treatment of adults and children asthma, including the prevention of daytime and nighttime asthma symptoms, the treatment of asthma patients who are aspirin-sensitive and prevention of exercise-induced bronchial contraction, it can also be used to relieve the seasonal allergic rhinitis symptoms of 15 year-old or over 15 year-old patients whose symptoms are invalid and intolerant to other treatment. Montelukast is a selective leukotriene receptor antagonist and has been approved for the oral administration treatment of asthma and allergic rhinitis. It is also a potent oral preparation that can significantly improve the inflammatory indicators. Biological determination of biochemistry and pharmacology has showed that montelukast sodium has a high affinity and selectivity to the CysLT1 receptors (compared with other kinds of pharmacologically important airway receptors such as prostanoid, cholinergic and β-adrenergic receptors). Montelukast can effectively suppress the physiological effects caused by the binding between LTC4, LTD4 and LTE4 receptor and CysLT1 receptor without any receptor agonistic activity. There is the secondary type of cysteinyl leukotriene receptor (CysLT2) presented in the lungs cysteinyl leukotriene receptor but may be limited to the blood vessels. So far, researchers haven’t cloned two receptors so the situation of CysLT receptor is illustrated through binding assay and pharmacological analysis. It has been now thought that montelukast does not antagonize CysLT2 receptors. The above information is edited by the lookchem of Dai Xiongfeng.

Uses

Different sources of media describe the Uses of 151767-02-1 differently. You can refer to the following data:
1. It can be applied to alleviate the symptoms caused by allergic rhinitis.
2. A selective leukotriene D4-receptor antagonist. Used as an antiasthmatic
3. antiinfective
4. A potent and highly selective CysLT1 receptor antagonist, without demonstrated CysLT2 activity
5. Montelukast sodium hydrate has been used as a positive control drug to study the protective effects of Gumiganghwal-tang aqueous extract (GGTA) against airway inflammation and pulmonary fibrosis.

Description

Montelukast was launched as Singulair in Mexico and Finland for the management of mild to moderate asthma inadequately controlled by inhaled corticosteroids and short-acting beta2-agonists. Montelukast can be obtained by an seven-step synthesis from 3-[2(E)-(7-chloroquinolin-2-yl)vinyl] benzaldehyde. Montelukast is a potent, selective and orally active antagonist of the CysLT1 (formerly called LTD4) receptor, thus blocking the effects of the cysteinyl leukotrienes LTC4, LTD4 and LTE4 on microvascular permeability and the activation of eosinophils. Montelukast represents the third molecule of this class which has been approved in asthma after pranlukast (1995) and zafirlukast (1996). Montelukast has been studied extensively in placebo-controlled clinical trials, in mildly or severe asthmatic patients challenged with LTD4 or exercise. A variety of acute bronchoconstricting challenges were inhibited or attenuated with all doses used. Montelukast demonstrated clinically significant improvements in the parameters of asthma control associated with an appreciable improvement in quality of life., reducing days with asthma exacerbations and allowing significant tapering of corticosteroids. Montelukast is well-tolerated and only needs to be administered once a day.

Chemical Properties

White or almost white, hygroscopic powder.

Manufacturing Process

Crotonaldehyde (3.23 mol) in 100 mL of 2-butanol was added dropwise to a refluxing solution of 4-chloroaniline (3.23 mol), p-chloranil (3.23 mol) and HCl conc. (808 mL) in 5.4 L of 2-butanol. After 2 hours of heating 2.7 L of solvent was removed under vacuum at 60°C. Then 2 L of toluene was added to the reaction mixture followed by removal of 2.5-3 L of solvent until a very pasty solid formed. THF (2 L) was added and the mixture heated 30 min after which it was cooled to 0°C. The solid was collected and washed with THF until pure by tlc. The solid was then dissolved in aq. K2CO3/EtOAc and the organic phase separated. The aqueous phase was extracted with EtOAc and the organic phases combined, dried over MgSO4 and the solvent removed. The product was crystallized in the minimum amount of EtOAc to give 328.08 g (57%) of 4-chloro-2-methylquinolin.4-Chloro-2-methylquinalin was converted into 3-(2-(7-chloro)-2- quinolinyl)ethenyl)benzaldehyde. Reaction was carried out according to a method described in U.S. Pat. No. 4,851,409To a degassed suspension of 3-(2-(7-chloro-2-quinolinyl)ethenyl)benzaldehyde (0.34 mol) in toluene (700 mL) at 0°C was added 1.0 M vinylmagnesium bromide in toluene/THF (370 mL). After stirring for 1 hour at 0°C, the reaction was quenched by the addition of saturated NH4Cl solution (150 ml), followed by H2O (500 mL) and HOAc (50 mL). The product was extracted with EtOAc and the two-phase system was filtered through celite to remove an insoluble precipitate. The aqueous phase was then re-extracted with EtOAc (100 mL) and the combined organic layer was washed with H2O, followed by brine. The solution was dried (MgSO4), and evaporated to give a dark yellow residue which was purified by flash chromatography (EtOAc:hexane 1:5, then 1:3). The product was filtered from the column fractions to give a solid of 1- (3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-2-propen-1-ol (melting point = 110-112°C). The filtrate was concentrated and the resulting residue was recrystallized from EtOAc/hexane 1:4 to give a second crop of 15.1 g.A degassed suspension of 1-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-2-propen-1-ol (46.6 mmol), n-Bu4NCl (93 mmol), LiOAcH2O (115 mmol), LiCl (93 mmol), Pd(OAc)2 (1.4 mmol) and methyl 2-(2-iodophenyl)propanoate in DMF (90 mL) was stirred for 2 hours at 100°C. The dark red solution was then cooled to 0°C and poured into saturated NaHCO3 solution (500 mL). The product was extracted with EtOAc and the organic layer was washed with H2O followed by brine. The solvent was removed under vacuum and the residue was purified by flash chromatography (EtOAc:hexane 1:10, 1:5 and 3:10) to give a pale yellow foam of ethyl 2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)ethenyl) phenyl)-3-hydroxy-propyl)benzoate (18.9 g).A mixture of anhydrous CeCl3 (164 mmol) in THF (500 mL) was refluxed overnight using a Dean Stark trap filled with activated molecular sieves. Methyl magnesium chloride (3.0 Molar solution in THF, 790 mmol) was added dropwise over 30 min to the CeCl3 slurry at 0°C. After stirring 2 hours, the mixture was cooled to -5°C and a toluene (600 mL) solution of the ethyl 2- (3(S)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-hydroxy-propyl)benzoate (152 mmol) was added dropwise over 1 hour. The reaction mixture was stirred another hour before the addition of 2 M HOAc (600 mL) and toluene (600 mL). The organic layer was washed with saturated aq. NaHCO3 and with brine. Concentration in vacuo and purification of the residue by flash chromatography (30% EtOAc in toluene) gave 63.48 g (91%) of the 2-(2- (3(S)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-hydroxypropyl)phenyl)-2- propanol.To a solution of BH3THF complex (1 M in THF, 262 mL) was added diethyl 1,1- cyclopropanedicarboxylate (134 mmol) at 25°C under N2. The solution was heated at reflux for 6 hours, cooled to r.t., and MeOH (300 mL) was cautiously added. The solution was stirred for 1 hour and then concentrated to an oil. The crude 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3- hydroxypropyl)phenyl)-2-propanol was dissolved in CH2Cl2 (234 mL) and SOCl2 (15.9 g, 134 mmol) was added dropwise over a period of 15 min at 25°C. After stirring for another 15 min, the mixture was washed with aqueous NaHCO3. The organic extract was dried over Na2SO4, filtered and concentrated to give quantitatively the 1,1-cyclopropanedimethanol cyclic sulfite.To a solution of the 1,1-cyclopropanedimethanol cyclic sulfite (99 mmol) in DMF (83 mL) was added NaCN (199 mmol). The mixture was heated to 90°C for 20 hours. Upon cooling, EtOAc (400 mL) was added and the solution was washed with saturated NaHCO3 solution (55 mL), H2O (4 times 55 mL), saturated NaCl solution and dried over Na2SO4. The solution was concentrated to give 7.1 g (65%) of 1-(hydroxymethyl)cyclopropaneacetonitrile.To a solution of 1-(hydroxymethyl)cyclopropaneacetonitrile (42 g, 378 mmol) in dry CH2Cl2 (450 mL) at -30°C was added Et3N (741 mmol) followed by CH3SO2Cl (562 mmol) dropwise. The mixture was warmed to 25°C, washed with NaHCO3, dried over Na2SO4 and concentrated in vacuo to give the corresponding mesylate. The mesylate was then dissolved in DMF (450 mL) and cooled to 0°C. Potassium thioacetate (55.4 g, 485 mmol) was added, and the mixture was stirred at 25°C for 18 hours. EtOAc (1.5 L) was added, the solution was washed with NaHCO3, dried over Na2SO4 and concentrated in vacuo to give 45 g (70%) of 1-(acetythiomethyl)cyclopropaneacetonitrile.To a solution of the 1-(acetythiomethyl)cyclopropaneacetonitrile (266 mmol) in MeOH (1.36 L) was added H2O (84 mL) and conc. H2SO4(168 mL). The mixture was heated to reflux for 20 hours, cooled to 25°C, H2O (1 L) was added and the product was extracted with CH2Cl2. The organic extract was washed with H2O and dried over Na2SO4. Concentration of the organic solution gave 36 g (93%) of the methyl 1-(thiomethyl)cyclopropaneacetate.To a solution of 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3- hydroxypropyl)phenyl)-2-propanol in THF was dissolved in THF (1 mL) and DMF (1 mL) at -40°C was added diisopropylethylamine (2.2 mmol) and then methanesulfonyl chloride (2.2 mmol). The mixture was stirred 2 hours with slow warming to -30°C. The methyl 1-(thiomethyl)cyclopropaneacetate (2.3 mmol) was added to the cloudy reaction mixture followed by dropwise addition of potassium tert-butoxide/THF solution (4.4 mmol). The reaction mixture was stirred at -30°C for 3.5 hours before quenching it with 25% aq NH4OAc. Extraction with EtOAc, washing the organic layer with brine and evaporation of the solvents left a residue that was purified by flash chromatography (5%-10% EtOAc in toluene) giving 658 mg (53%) of methyl 1-((((R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(2-hydroxy-2- propyl)phenyl)propyl)thio)methyl)cyclopropaneacetate.Following the hydrolysis the methyl 1-((((R)-(3-(2-(7-chloro-2-quinolinyl) ethenyl)phenyl)-3-(2-(2-hydroxy-2-propyl)phenyl)propyl)thio)methyl) cyclopropaneacetate with NaOH was obtained the free acid: 4-((1(R)-(3-(2-(7- chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(2-hydroxy-2-propyl)-phenyl)propyl) thio)methyl)cyclopropaneacetic acid or sodium 1-(((1(R)-(3-(2-(7-chloro-2- quinolinyl)ethenyl)phenyl)-3-(2-(2-hydroxy-2-propyl)phenyl)propyl)thio) methyl) cyclopropaneacetate.

Brand name

Singulair (Merck).

Therapeutic Function

Anti-asthmatic

Biochem/physiol Actions

Montelukast sodium hydrate is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is a subtype specific CysLT1 receptor antagonist.

References

1) Lynch?et al.?(1999),?Characterization of the human cysteinyl leukotriene CysLT1 receptor; Nature,?399?789 2) Jones?et al. (1995),?Pharmacology of montelukast sodium (Singulair), a potent and selective leukotriene D4 receptor antagonist; Can. J. Physiol. Pharmacol.,?73?191 3) Reiss?et al.?(1998),?Montelukast, a once-daily leukotriene receptor antagonist, in the treatment of chronic asthma: a multicenter, randomized, double-blind trial. Montelukast Clinical Research Study Group; Arch. Intern. Med.,?158?1213 4) Zhao?et al.?(2011),?Montelukast, a cysteinyl leukotriene receptor-1 antagonist, attenuates chronic brain injury after focal cerebral ischaemia in mice and rats; J. Pharm. Pharmacol.,?63?550 5) Lenz?et al.?(2014),?Cysteinyl leukotriene receptor (CysLT) antagonists decrease pentylenetetrazol-induced seizures and blood-brain barrier dysfunction; Neuroscience,?277?859 6) Huber?et al.?(2011)?Inhibition of leukotriene receptors boosts neural progenitor proliferation; Cell Physiol. Biochem.,?28?793

Check Digit Verification of cas no

The CAS Registry Mumber 151767-02-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,1,7,6 and 7 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 151767-02:
(8*1)+(7*5)+(6*1)+(5*7)+(4*6)+(3*7)+(2*0)+(1*2)=131
131 % 10 = 1
So 151767-02-1 is a valid CAS Registry Number.
InChI:InChI=1/C35H36ClNO3S.Na/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29;/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39);/q;+1/p-1/b15-10+;

151767-02-1 Well-known Company Product Price

  • Brand
  • (Code)Product description
  • CAS number
  • Packaging
  • Price
  • Detail
  • TCI America

  • (M2340)  Montelukast Sodium Hydrate  >98.0%(HPLC)(T)

  • 151767-02-1

  • 200mg

  • 590.00CNY

  • Detail
  • TCI America

  • (M2340)  Montelukast Sodium Hydrate  >98.0%(HPLC)(T)

  • 151767-02-1

  • 1g

  • 1,890.00CNY

  • Detail
  • Sigma-Aldrich

  • (PHR1603)  Montelukast Sodium  pharmaceutical secondary standard; traceable to USP, PhEur

  • 151767-02-1

  • PHR1603-1G

  • 1,078.62CNY

  • Detail
  • Sigma-Aldrich

  • (Y0001435)  Montelukast for peak identification  European Pharmacopoeia (EP) Reference Standard

  • 151767-02-1

  • Y0001435

  • 1,880.19CNY

  • Detail
  • USP

  • (1446859)  Montelukast sodium  United States Pharmacopeia (USP) Reference Standard

  • 151767-02-1

  • 1446859-50MG

  • 4,662.45CNY

  • Detail

151767-02-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 10, 2017

Revision Date: Aug 10, 2017

1.Identification

1.1 GHS Product identifier

Product name montelukast sodium

1.2 Other means of identification

Product number -
Other names sodium,2-[1-[[(1R)-1-[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanylmethyl]cyclopropyl]acetate

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:151767-02-1 SDS

151767-02-1Synthetic route

sodium hydroxide
1310-73-2

sodium hydroxide

montelukast
158966-92-8

montelukast

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
In methanol; toluene at 20℃; for 1h; Product distribution / selectivity;100%
In methanol; toluene at 2 - 20℃; for 0.75h; Product distribution / selectivity;100%
In methanol at 20℃; for 1h; Product distribution / selectivity;73%
In methanol at 25 - 35℃; for 0.166667h;
montelukast
158966-92-8

montelukast

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium hydroxide In methanol; toluene at 20℃; for 1h;100%
With sodium hydroxide In methanol; water; toluene for 0.5h; Product distribution / selectivity; Alkaline aqueous solution;98%
With sodium hydroxide In methanol at -5 - 35℃; for 1h;98.7%
1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt
577953-88-9

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt With acetic acid In dichloromethane pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt With acetic acid In dichloromethane; water pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt With acetic acid In water; toluene at 20℃; for 0.166667h; Inert atmosphere;
Stage #2: With sodium hydroxide In methanol at 20 - 25℃; for 2h; Inert atmosphere;
94%
1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid α-methylbenzylamine salt
880769-29-9

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid α-methylbenzylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid α-methylbenzylamine salt With acetic acid In dichloromethane pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid α-methylbenzylamine salt With acetic acid In dichloromethane; water pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid α-methylbenzylamine salt With acetic acid In dichloromethane; water at 25 - 35℃; for 0.75h;
Stage #2: With sodium hydroxide In ethanol; dichloromethane at 25 - 30℃; for 1h; Product distribution / selectivity;
75.6%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid α-methylbenzylamine salt With acetic acid In dichloromethane; water at 25 - 35℃;
Stage #2: With sodium hydroxide In ethanol at 25 - 30℃; Product distribution / selectivity;
75.6%
1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt
1100021-03-1

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt With acetic acid In dichloromethane; water pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid benzylamine salt With acetic acid In dichloromethane pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-chloro benzylamine salt
1254938-23-2

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-chloro benzylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-chloro benzylamine salt With acetic acid In dichloromethane pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-chloro benzylamine salt With acetic acid In dichloromethane; water pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-methoxy benzylamine salt

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-methoxy benzylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-methoxy benzylamine salt With acetic acid In dichloromethane pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-methoxy benzylamine salt With acetic acid In dichloromethane; water pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
99%
sodium hydroxide
1310-73-2

sodium hydroxide

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt
577953-88-9

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid dicyclohexylamine salt With water; acetic acid In toluene at 20 - 25℃; for 0.166667h;
Stage #2: sodium hydroxide In ethanol; water; toluene at 20℃; for 0.333333h;
98%
1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-bromo benzylamine salt
1254938-26-5

1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-bromo benzylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-bromo benzylamine salt With acetic acid In dichloromethane pH=4 - 4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
98%
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinil)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropane acetic acid 4-bromo benzylamine salt With acetic acid In dichloromethane; water pH=4.5;
Stage #2: With pyrographite; sodium hydroxide In methanol; water for 1h;
98%
1-(((1-(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropylacetate 2-amino-1-butanol

1-(((1-(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropylacetate 2-amino-1-butanol

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1-(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)cyclopropylacetate 2-amino-1-butanol With acetic acid In dichloromethane; water for 0.25h;
Stage #2: With pyrographite; sodium sulfate; sodium hydroxide In methanol at 15 - 25℃; for 1h; Temperature;
97.2%
montelukast isopropylamine salt
918972-53-9

montelukast isopropylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium t-butanolate In toluene at 30 - 35℃; for 0.75h; Product distribution / selectivity; Inert atmosphere; Darkness;94%
With sodium t-butanolate In toluene at 35℃;78%
Stage #1: montelukast isopropylamine salt With hydrogenchloride In dichloromethane; water at 10 - 25℃; for 0.5h; pH=4 - 4.5;
Stage #2: With sodium hydroxide In ethanol; dichloromethane at 8 - 12℃; for 2h;
Stage #1: montelukast isopropylamine salt With hydrogenchloride In dichloromethane; water at 10 - 20℃; pH=4 - 4.5; Inert atmosphere;
Stage #2: With sodium hydroxide In ethanol; dichloromethane at 8 - 12℃; for 30h; Inert atmosphere;
1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid R-(+)-α-methylbenzylamine salt

1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid R-(+)-α-methylbenzylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium methylate; pyrographite In toluene at 25 - 30℃; for 1.5h;93%
1-(((1-(R)-(3-(2-(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl) thio)methyl)cyclopropaneacetic acid dipropylamine salt
880769-26-6

1-(((1-(R)-(3-(2-(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl) thio)methyl)cyclopropaneacetic acid dipropylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1-(R)-(3-(2-(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl) thio)methyl)cyclopropaneacetic acid dipropylamine salt With acetic acid In water; isopropyl alcohol at 4 - 40℃; for 17h; Inert atmosphere;
Stage #2: With sodium hydroxide In methanol for 1h;
92%
Stage #1: 1-(((1-(R)-(3-(2-(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl) thio)methyl)cyclopropaneacetic acid dipropylamine salt With acetic acid In dichloromethane; water at 25 - 30℃; for 0.75h;
Stage #2: With sodium hydroxide In ethanol; dichloromethane at 25 - 30℃; for 1h; Product distribution / selectivity;
67.8%
Stage #1: 1-(((1-(R)-(3-(2-(E)-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl) thio)methyl)cyclopropaneacetic acid dipropylamine salt With acetic acid In dichloromethane; water at 25 - 35℃;
Stage #2: With sodium hydroxide In ethanol at 25 - 30℃; Product distribution / selectivity;
67.8%
cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate
142522-28-9

cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium hydroxide In methanol at 20℃; for 0.5h; Inert atmosphere;92%
montelukast N-methyl-morpholine salt
942303-96-0

montelukast N-methyl-morpholine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium methylate In toluene at 25 - 30℃; for 0.5h;90%
montelukast hexamethylenediamine

montelukast hexamethylenediamine

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: montelukast hexamethylenediamine With tartaric acid In dichloromethane; water for 0.25 - 0.333333h;
Stage #2: With sodium hydroxide In methanol; dichloromethane for 0.0833333 - 0.166667h;
90%
(R,E)-2-(1-((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)-phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propylthio)-methyl)cyclopropyl)acetic acid L-(-)-ephedrine

(R,E)-2-(1-((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)-phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propylthio)-methyl)cyclopropyl)acetic acid L-(-)-ephedrine

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: (R,E)-2-(1-((1-(3-(2-(7-chloroquinolin-2-yl)vinyl)-phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propylthio)-methyl)cyclopropyl)acetic acid L-(-)-ephedrine With acetic acid In dichloromethane; water pH=7; Inert atmosphere;
Stage #2: With sodium hydroxide In methanol for 1h; Activated carbon;
86.8%
Montelukast L-ephedrine salt
1312993-47-7

Montelukast L-ephedrine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: Montelukast L-ephedrine salt With acetic acid In dichloromethane; water at 15 - 20℃; pH=7; Inert atmosphere;
Stage #2: With sodium hydroxide In methanol at 32℃;
86.8%
montelukast n-propylamine salt
1100021-00-8

montelukast n-propylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium t-butanolate In toluene at 30℃;82%
montelukast tert-butylamine salt
851755-58-3

montelukast tert-butylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: montelukast tert-butylamine salt With acetic acid In dichloromethane; water for 0.5h; Industry scale;
Stage #2: With sodium hydroxide In methanol for 0.333333h; Industry scale;
75.4%
With sodium methylate In methanol at 25 - 35℃; for 1h; Product distribution / selectivity;
Stage #1: montelukast tert-butylamine salt With acetic acid In dichloromethane; water at 25 - 35℃; for 0.25h;
Stage #2: With sodium hydroxide; pyrographite In methanol at 25 - 35℃; for 0.5h;
[R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid homoveratrylamine salt
1187364-41-5

[R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid homoveratrylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid homoveratrylamine salt With acetic acid In dichloromethane; water at 0 - 5℃;
Stage #2: With sodium hydroxide In methanol at 25 - 35℃; Product distribution / selectivity;
75%
C39H43ClN2O2S
1020313-99-8

C39H43ClN2O2S

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium hydroxide; water; ethylene glycol at 120 - 195℃; for 3 - 25h; Product distribution / selectivity;60%
(1-{1-(R)-(E)-{3-[2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propylsulfanylmethyl}-cyclopropyl)-acetic acid diisobutylamine salt
1399184-58-7

(1-{1-(R)-(E)-{3-[2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propylsulfanylmethyl}-cyclopropyl)-acetic acid diisobutylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium tert-pentoxide In methyl cyclohexane; toluene at 20 - 45℃; for 1.5h;56%
With sodium tert-pentoxide In toluene at 40 - 45℃; for 0.5h; Product distribution / selectivity; Inert atmosphere;56%
1-(((1(R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)-phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)-cyclopropaneacetic acid trans-4-aminocyclohexanol salt
1008509-41-8

1-(((1(R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)-phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)-cyclopropaneacetic acid trans-4-aminocyclohexanol salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-(((1(R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)-phenyl)-3-(2-(1-hydroxy-1-methylethyl)phenyl)propyl)thio)methyl)-cyclopropaneacetic acid trans-4-aminocyclohexanol salt With tartaric acid In water for 1h;
Stage #2: With sodium hydroxide In methanol for 1h; Product distribution / selectivity;
1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid cyclohexylamine salt
945934-73-6

1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid cyclohexylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]sulfanyl]methyl]cyclopropaneacetic acid cyclohexylamine salt With tartaric acid In water for 1h;
Stage #2: With sodium hydroxide In methanol for 1h; Product distribution / selectivity;
1-[[[(1R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl] cyclopropane acetic acid magnesium salt

1-[[[(1R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl] cyclopropane acetic acid magnesium salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
Stage #1: 1-[[[(1R)-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl] cyclopropane acetic acid magnesium salt With acetic acid In water at 25 - 30℃; for 0.5h;
Stage #2: With sodium hydroxide In ethanol; water at 25 - 30℃; for 0.5h;
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 methyl ester
855473-51-7

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 methyl ester

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
With sodium hydroxide In tetrahydrofuran; methanol; water at 24 - 27℃; for 20h; Product distribution / selectivity; Alkaline aqueous solution;
With sodium hydroxide In tetrahydrofuran; methanol at 20 - 25℃; for 50h;
With sodium hydroxide In tetrahydrofuran; ISOPROPYLAMIDE at 40℃; for 4h;
sodium hydroxide
1310-73-2

sodium hydroxide

montelukast tert-butylamine salt
851755-58-3

montelukast tert-butylamine salt

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
In methanol at 5 - 10℃; for 0.5h; Product distribution / selectivity;
sodium hydroxide
1310-73-2

sodium hydroxide

n-butylamine salt of montelukast
1028683-07-9

n-butylamine salt of montelukast

Montelukast sodium
151767-02-1

Montelukast sodium

Conditions
ConditionsYield
In methanol at 5 - 10℃; for 0.5h; Product distribution / selectivity;
Montelukast sodium
151767-02-1

Montelukast sodium

montelukast
158966-92-8

montelukast

Conditions
ConditionsYield
With hydrogenchloride In water at 20 - 25℃; for 1h;97%
With hydrogenchloride In water at 20℃; for 1h; pH=6;97.9%
With hydrogenchloride; citric buffer In water; acetone at 20 - 25℃; for 2h;76%
3,4,5-trifluorophenylboronic acid
143418-49-9

3,4,5-trifluorophenylboronic acid

Montelukast sodium
151767-02-1

Montelukast sodium

C41H38F3NO3S

C41H38F3NO3S

Conditions
ConditionsYield
With O4P(3-)*3K(1+)*5H2O; tris(1-adamantyl)phosphine; C28H26N2O8Pd2S2 In tetrahydrofuran at 100℃; for 5h; Suzuki-Miyaura Coupling; Inert atmosphere; Schlenk technique;89%
3,4,5-trifluorophenylboronic acid
143418-49-9

3,4,5-trifluorophenylboronic acid

Montelukast sodium
151767-02-1

Montelukast sodium

C41H38F3NO3S

C41H38F3NO3S

Conditions
ConditionsYield
With O4P(3-)*3K(1+)*5H2O; tris(1-adamantyl)phosphine; {2-[((acetyl-κO)amino)phenyl-κC](tri-1-adamantylphosphine)palladium}(p-toluenesulfonate) In tetrahydrofuran at 100℃; for 5h; Suzuki-Miyaura Coupling; Inert atmosphere;89%
dimethyl sulfate
77-78-1

dimethyl sulfate

Montelukast sodium
151767-02-1

Montelukast sodium

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 methyl ester
855473-51-7

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 methyl ester

Conditions
ConditionsYield
With sodium hydroxide In 1,4-dioxane Reflux;54%
Montelukast sodium
151767-02-1

Montelukast sodium

[R,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]-phenyl]-3-[2-(-hydroxy-1-methylethyl) phenyl]propyl]-sulfinyl] methyl] cyclopropaneacetic acid

[R,E]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl) ethenyl]-phenyl]-3-[2-(-hydroxy-1-methylethyl) phenyl]propyl]-sulfinyl] methyl] cyclopropaneacetic acid

Conditions
ConditionsYield
With 3-chloro-benzenecarboperoxoic acid; trifluoroacetic acid In dichloromethane at -22℃; for 2h; Yield given;
Stage #1: Montelukast sodium With dihydrogen peroxide In methanol; water for 3h;
Stage #2: With acetic acid
With dihydrogen peroxide In methanol; water for 3h;

151767-02-1Upstream product

151767-02-1Relevant articles and documents

Preparation method of montelukast sodium

-

Paragraph 0054-0074; 0083-0086, (2020/12/15)

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.

Synthesis method of montelukast sodium

-

Paragraph 0020; 0050-0067, (2020/11/23)

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%.

Montelukast sodium intermediate and preparation method and application thereof

-

Paragraph 0104; 0105; 0106, (2017/08/31)

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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