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PEMIROLAST

Product Name
PEMIROLAST
CAS No.
69372-19-6
Chemical Name
PEMIROLAST
Synonyms
Hsdb 7291;Pemilaston;PEMIROLAST;Pemirolastum;Unii-2C09nv773m;Pemirolast [inn];Pemiroplastpotassium;PEMIROLAST USP/EP/BP;Pemirolastum [inn-latin];100299-08-9 (Potassium salt)
CBNumber
CB6140326
Molecular Formula
C10H8N6O
Formula Weight
228.21
MOL File
69372-19-6.mol
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PEMIROLAST Property

Melting point:
310-311° (dec)
Boiling point:
454.8±55.0 °C(Predicted)
Density 
1?+-.0.1 g/cm3(Predicted)
pka
4.00±0.50(Predicted)
CAS DataBase Reference
69372-19-6(CAS DataBase Reference)
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Safety

Hazardous Substances Data
69372-19-6(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
API0016548
Product name
9-METHYL-3-(1H-TETRAAZOL-5-YL)-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE
Purity
95.00%
Packaging
5MG
Price
$499.69
Updated
2021/12/16
AHH
Product number
MT-57697
Product name
Pemirolast
Purity
98%
Packaging
1g
Price
$330
Updated
2021/12/16
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PEMIROLAST Chemical Properties,Usage,Production

Originator

Alamast, Santen

Uses

Anti-allergic; inhibitor (mediator release).

Definition

ChEBI: Pemirolast is a pyridopyrimidine.

Manufacturing Process

Ferrous nitrate hexahydrate (60 mg) followed by sodium (4.5 g, 0.196 gatom) were added to liquid ammonia. To this mixture was added a solution of 3-methylpyridine (10.0 g, 0.093 mole) in N,N-dimethylaniline (21 ml) over a period of 5 min. The ammonia was allowed to evaporate and the residue heated under nitrogen by means of an oil bath maintained at 180°C for 18 h. The cooled residue was treated with ice (50 g) followed by 2 N sodium hydroxide (50 ml). The mixture was triturated for 2 h and then filtered. The collected solid was washed with boiling toluene (2 times 100 ml). The toluene layer was separated from the combined filtrate and washings, concentrated to about 50 ml and extracted with 5% aqueous acetic acid (5 times 20 ml). The combined extracts were filtered and reduced to dryness. The residue was recrystallized from methylcyclohexane to give 2-amino-3-methylpyridine acetate (4.9 g, 29%), melting point 85°-95°C. The acetate (2.5 g, 1.37 mmoles) was briefly suspended in 1 N sodium hydroxide (50 ml). The mixture was extracted with methylene chloride. The extract was washed with water, dried, and concentrated to give 2-amino-3-methylpyridine as an oil.
A solution of 2-amino-3-methylpyridine (5.0 g, 0.0462 mole) and ethyl ethoxymethylenecyanoacetate (7.82 g, 0.0462 mole) in toluene (4 ml) was heated for 15 min by means of an oil bath maintained at 100°C. The solution was cooled and the crude product (9.1 g, 85%) collected by filtration. The product was recrystallized from 2-propanol to give an analytical sample of ethyl 2-cyano-3-(3-methyl-2-pyridylamino)acrylate, melting point 144°146°C.
Aluminum chloride (3.51 g, 0.0263 mole) was added to cold (-30°C) tetrahydrofuran (180 ml). Sodium azide (5.12 g, 0.0788 mole) was added and the mixture heated under reflux for 30 min. The mixture was cooled to 5°C. Ethyl 2-cyano-3-(3-methyl-2-pyridylamino)acrylate (5.0 g, 0.0216 mole) was added and the mixture heated under reflux for 18 h. The tetrahydrofuran was removed under reduced pressure. The residue was treated with ice water (100 ml) and acidified to pH 3 with 6 N hydrochloric acid. The mixture was filtered and the collected solid recrystallized from N,N-dimethylformamide to give the 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (2.5 g, 50.7%). Melting point 310°-311°C, dec.
Potassium hydroxide was added dropwise to a stirred mixture of 9-methyl-3(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one in water .The mixture was diluted with water to a volume of about 300 ml and was then heated to a temperature of 50°C during 2 min. The mixture was filtered and the water removed from the filtrate by lyophilization. The residue was recrystallized from water:ethanol to give the 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2 2632 a]pyrimidin-4-one potassium salt

brand name

Alamast (Sanofi Winthrop).

Therapeutic Function

Antiallergic, Antiulcer

Clinical Use

Pemirolast, with an acidic tetrazole isosteric replacement for a carboxylic acid functionality, is used topically in the eye to prevent itching associated with allergic conjunctivitis. It is an inhibitor of the release of histamine and other inflammatory mediators, including leukotrienes. Significant use as a systemic agent has been reported, and it has been shown to be of value in preventing restenosis after percutaneous coronary angiopathy.

PEMIROLAST Preparation Products And Raw materials

Raw materials

Preparation Products

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PEMIROLAST Suppliers

Pure Chemistry Scientific Inc.
Tel
001-857-928-2050 or 1-888-588-9418
Fax
001-617-206-9595
Email
sales@chemreagents.com
Country
United States
ProdList
10186
Advantage
62
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Tel
0755-4000505016 13380397412
Fax
0755 28094224
Email
3001272453@qq.com
Country
China
ProdList
5047
Advantage
50
Hangzhou Sage Chemical Co., Ltd.
Tel
+86057186818502 13588463833
Fax
Pls mail us for more information!
Email
info@sagechem.com
Country
China
ProdList
10266
Advantage
58
China Nobel Chem Co., Limited
Tel
+86(0)21 60484900
Fax
+86(0)21 60484900
Country
China
ProdList
764
Advantage
50
ChemStrong Scientific Co.,Ltd
Tel
0755-0755-66853366 13670046396
Fax
0755-28363542
Email
sales@chem-strong.com
Country
China
ProdList
18042
Advantage
56
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Zhengzhou Acme Chemical Co., Ltd.
Tel
0371-037163312495,13303845143 13303845143
Fax
QQ3001379618
Email
3001379618@qq.com
Country
China
ProdList
9992
Advantage
58
Shanghai Pin Research Chemical Co., Ltd.
Tel
15900489257
Email
271793832@qq.com
Country
China
ProdList
36
Advantage
58
Dayang Chem (Hangzhou) Co.,Ltd.
Tel
571-88938639 +8617705817739
Fax
+86-571-88938652,+86-571- 88492614
Email
info@dycnchem.com
Country
China
ProdList
52849
Advantage
58
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View Lastest Price from PEMIROLAST manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
PEMIROLAST 69372-19-6
Price
US $1.00-1.00/KG
Min. Order
1g
Purity
99%
Supply Ability
50tons
Release date
2020-05-08
Dideu Industries Group Limited
Product
PEMIROLAST 69372-19-6
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons Min
Release date
2021-06-16

69372-19-6, PEMIROLASTRelated Search:


  • PEMIROLAST
  • Pemiroplastpotassium
  • 9-Methyl-3-(1H-tetrazol-5-y1)-4H-pyrido[1,2-α]pyrimidin-4-one
  • Pemilaston
  • 9-Methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one
  • 100299-08-9 (Potassium salt)
  • 4H-Pyrido(1,2-A)pyrimidin-4-one, 9-methyl-3-(1H-tetrazol-5-yl)-
  • Hsdb 7291
  • Pemirolast [inn]
  • Pemirolastum
  • Pemirolastum [inn-latin]
  • Unii-2C09nv773m
  • 4H-Pyrido[1,2-a]pyrimidin-4-one,9-methyl-3-(2H-tetrazol-5-yl)-
  • PEMIROLAST USP/EP/BP
  • 9-methyl-3-(2H-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one
  • 69372-19-6
  • C10H8N6O