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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
Molecular Weight:
228.21
MDL Number:
MFCD00864611
MOL File:
69372-19-6.mol
MSDS File:
SDS
Last updated:2023-05-04 17:34:41

PEMIROLAST Properties

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)
EWG's Food Scores 1
FDA UNII 2C09NV773M

PEMIROLAST price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
American Custom Chemicals Corporation API0016548 9-METHYL-3-(1H-TETRAAZOL-5-YL)-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE 95.00% 69372-19-6 5MG $499.69 2021-12-16 Buy
AHH MT-57697 Pemirolast 98% 69372-19-6 1g $330 2021-12-16 Buy
Product number Packaging Price Buy
API0016548 5MG $499.69 Buy
MT-57697 1g $330 Buy

PEMIROLAST Chemical Properties,Uses,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.

102781-19-1
69372-19-6
Synthesis of PEMIROLAST from 4-Imino-9-methyl-4H-pyrido[1,2-a]pyrimidine-3-carbonitrile

PEMIROLAST Suppliers

Global( 46)Suppliers
Supplier Tel Email Country ProdList Advantage
Shaanxi Dideu Medichem Co. Ltd
+86-29-87569265 +86-18612256290 1056@dideu.com China 3632 58
Career Henan Chemica Co
+86-0371-86658258 15093356674; laboratory@coreychem.com China 30255 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 29271 58
Dayang Chem (Hangzhou) Co.,Ltd.
571-88938639 +8617705817739 info@dycnchem.com CHINA 52867 58
Hebei Duling International Trade Co. LTD
+8618032673083 sales05@hbduling.cn China 15745 58
ZHEJIANG JIUZHOU CHEM CO., LTD
+86-0576225566889 +86-13454675544 admin@jiuzhou-chem.com;jamie@jiuzhou-chem.com;alice@jiuzhou-chem.com China 20000 58
GIHI CHEMICALS CO.,LIMITED
+8618058761490 info@gihichemicals.com China 49999 58
Amadis Chemical Company Limited
571-89925085 sales@amadischem.com China 131981 58
Mainchem Co., Ltd. +86-0592-6210733 sale@mainchem.com China 32360 55
Pure Chemistry Scientific Inc. 001-857-928-2050 or 1-888-588-9418 sales@chemreagents.com United States 10194 62

View Lastest Price from PEMIROLAST manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
PEMIROLAST pictures 2022-10-19 PEMIROLAST
69372-19-6
US $50.00 / kg 1kg 99% 1 Hebei Duling International Trade Co. LTD
PEMIROLAST pictures 2021-07-20 PEMIROLAST
69372-19-6
US $1.00-1.00 / KG 1g 99% 50tons Shaanxi Dideu Medichem Co. Ltd
PEMIROLAST USP/EP/BP pictures 2021-06-17 PEMIROLAST USP/EP/BP
69372-19-6
US $1.10 / g 1g 99.9% 100 Tons Min Dideu Industries Group Limited
  • PEMIROLAST pictures
  • PEMIROLAST
    69372-19-6
  • US $50.00 / kg
  • 99%
  • Hebei Duling International Trade Co. LTD
  • PEMIROLAST pictures
  • PEMIROLAST
    69372-19-6
  • US $1.00-1.00 / KG
  • 99%
  • Shaanxi Dideu Medichem Co. Ltd
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