ChemicalBook > CAS DataBase List > Epinastine

Epinastine

Product Name: Epinastine
CAS No.: 80012-43-7
Chemical Name: Epinastine
Synonyms: WAL801;CS-1366;Epastine;EPINASTINE;ELESTAT;WAL801;Apinastine Base;EPINASTINE BASE;Epinastine (WAL801);Epinastine USP/EP/BP;Epinastine in methanol
CBNumber: CB2230197
Molecular Formula: C16H15N3
Formula Weight: 249.31
MOL File: 80012-43-7.mol

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Epinastine Property

Melting point:: 205-208°
Boiling point:: 428.0±55.0 °C(Predicted)
Density: 1.32±0.1 g/cm3(Predicted)
storage temp.: Keep in dark place,Inert atmosphere,Room temperature
solubility: DMSO : ≥ 50 mg/mL (200.55 mM);Water : < 0.1 mg/mL (insoluble)
pka: 11.2(at 25℃)
form: Solid
color: White to off-white
CAS DataBase Reference: 80012-43-7(CAS DataBase Reference)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H372Causes damage to organs through prolonged or repeated exposure

H411Toxic to aquatic life with long lasting effects

Precautionary statements

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

TCI Chemical

Product number: E1540
Product name: Epinastine
Packaging: 200MG
Price: $130
Updated: 2025/07/31

TCI Chemical

Product number: E1540
Product name: Epinastine
Packaging: 1G
Price: $390
Updated: 2025/07/31

TRC

Product number: E588715
Product name: Epinastine
Packaging: 100mg
Price: $600
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0002565
Product name: EPINASTINE
Purity: 95.00%
Packaging: 100MG
Price: $885.31
Updated: 2021/12/16

AK Scientific

Product number: G296
Product name: Epinastine
Packaging: 50mg
Price: $128
Updated: 2021/12/16

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Epinastine Chemical Properties,Usage,Production

Description

Epinastine hydrochloride, an orally active antihistaminic agent, was marketed in Japan for the treatment of bronchial asthma, allergic rhinitis, urticaria, eczema, dermatitis, and psoriasis vulgaris.Epinastine is one of the most effective peripherally acting histamine H₁-receptor antagonists without sedative effects.In addition, it exhibits potent anti-PAF and anti-LT activity which may also contribute significantly to its antiallergic activity. Chronic epinastine has been reported to effectively inhibit airway hyper-responsiveness in rats. Potent inhibitory effects of epinastine on bronchoconstriction induced by histamine and bradykinin, but not by other chemical mediators, has also been reported. Studies have indicated that there are no significant differences in pharmacological properties among D-, L-, and racemic epinastine.

Originator

Boehringer lngelheim (Germany)

Uses

Epinastine is antihistamine and mast cell stabilize that is used in eye drops for the treatment of allergic conjunctivitis.

Definition

ChEBI: A benzazepine that is 6,11-dihydro-5H-dibenzo[b,e]azepine in which the azepine ring is fused to the e side of 4,5-dihydro-1H-imidazol-2-amine.

brand name

Aleslon

Clinical Use

Epinastine is a potent, long-acting H1 antihistamine and an inhibitor of the release of histamine and other transmitters from mast cells. It has some affinity for H2 receptors as well. It is used as an eye drop for allergic conjunctivitis. It does not penetrate into the CNS and is classified as a nonsedating antihistamine.

Synthesis

Several patents on the synthesis of epinastin (VIII) have appeared in Europe and Japan. The synthesis described below is taken partly from the US patent and a Japanese patent. All the syntheses utilized 6-aminomethyl-6,11-dihydro-5H-dibenzo[b.e]azepine (80) as the key intermediate which was converted to the final guanidine epinastine by reacting with cyanogen bromide. The solution of 80 in ethanol was treated with a solution of cyanogen bromide in THF at room temperature and stirred overnight. The hydrobromide salt was collected in 79% yield after adding ether to the reaction mixture. The salt was free based with a solution of sodium hydroxide and then treated with an ethereal solution of HCl to obtain the epinastine hydrochloride salt VIII. For the preparation of the key intermediate, chloroimine 78, presumably obtained from ketone 77 via Beckmann rearrangement, was reacted with sodium cyanide in DMSO to give the nitrile 79 in 70% yield. Reduction of the imino nitrile was carried out in THF in the presence of an acid with LAH to give the key intermediate 80 in 67% yield.
An alternate approach to preparation of 80 is shown in Scheme 8 as well. Reaction of the commercially available chloride 81 with phthalimide in the presence of a base gave the phthalimide 82. Reduction of the imine with sodium borohydride gave 83, which was then reacted with hydrazine hydrate to free up the amine in 90% yield. The amine intermediate was isolated as the fumarate salt.

Epinastine Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Epinastine manufacturers

Shandong Xuhuang New material CoLTD

Product: epinastine 80012-43-7
Price: US $120.00/KG
Min. Order: 1KG
Purity: 99.99%
Supply Ability: 100KG
Release date: 2025-02-25

Shaanxi Dideu Medichem Co. Ltd

Product: Epinastine 80012-43-7
Price: US $1.00-1.00/KG
Min. Order: 1g
Purity: 99%
Supply Ability: 50tons
Release date: 2020-05-08

WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD

Product: Epinastine 80012-43-7
Price: US $0.00/KG
Min. Order: 1g
Purity: 99%
Supply Ability: 100kg
Release date: 2020-10-28

80012-43-7, EpinastineRelated Search:

Glycine AMINOACETONITRILE HYDROGEN SULFATE EPINASTINE HYDROCHLORIDE,EPINASTINE HCL Betaine ALTRENOGEST Dihydromyrcenol EPINASTINE HCL epinastine hydrobromide 6-Aminomethyl-5,6-dihydromorphanthridine Imidazole 6,11-DIHYDRO-5H-DIBENZO[B,E]AZEPINE N-O-TOLYL-GUANIDINE N1,N1-DIMETHYL-1-(2-METHYLPHENYL)-1,2-ETHANEDIAMINE 9,13b-Dehydro Epinastine Hydrochloride AMINO ACIDS Nitrogen and hydrogen mixed gas Epinastine Epinastine Hydrochloride/Free base

3-amino-9,13b-dihydro-1h-dibenz[c,f]imidazo[1,5-a]azepine

EPINASTINE

EPINASTINE BASE

9,13b-Dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3- amine

Apinastine Base

3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine

CS-1366

ELESTAT;WAL801

WAL801

1H-Dibenz[c,f]imidazo[1,5-a]azepin-3-amine, 9,13b-dihydro-

Epinastine USP/EP/BP

Epinastine (WAL801)

EpinastineQ: What is Epinastine Q: What is the CAS Number of Epinastine Q: What is the storage condition of Epinastine

9,13b-Dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine

Epinastine in methanol

2,4-diazatetracyclo[12.4.0.02,?.0?,12]octadeca-1(14),3,7(12),8,10,15,17-heptaen-3-amine

Epastine

9,13b-Dihydro-1H-dibenz(c,f)imidazo(1,5a)azepin-3-amin

80012-43-7

80012-43-07

C16H15N3