BEPOTASTINE BESILATE

ChemicalBook > CAS DataBase List > BEPOTASTINE BESILATE

Product Name: BEPOTASTINE BESILATE
CAS No.: 190786-44-8
Chemical Name: BEPOTASTINE BESILATE
Synonyms: BB;CS-645;CS-487;Talion;Bepreve;TAU 284;Talion (TN);Benzestatine;Betastine besylate;BEPOTASTINE BESILATE
CBNumber: CB9810068
Molecular Formula: C27H31ClN2O6S
Formula Weight: 547.06
MOL File: 190786-44-8.mol

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BEPOTASTINE BESILATE Property

Melting point:: 161-163°
alpha: D20 +6.0° (c = 5 in methanol)
storage temp.: Inert atmosphere,Room Temperature
solubility: DMSO (Slightly, Heated), Methanol (Slightly, Heated)
form: Solid
color: White to Light Beige
Stability:: Hygroscopic

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23721
Product name: Bepotastine (besylate)
Purity: ≥95%
Packaging: 5mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 23721
Product name: Bepotastine (besylate)
Purity: ≥95%
Packaging: 10mg
Price: $78
Updated: 2024/03/01

Cayman Chemical

Product number: 23721
Product name: Bepotastine (besylate)
Purity: ≥95%
Packaging: 25mg
Price: $172
Updated: 2024/03/01

Usbiological

Product number: 003877
Product name: Bepotastine Besylate
Packaging: 5mg
Price: $425
Updated: 2021/12/16

TRC

Product number: B317000
Product name: (S)-BepotastineBesylate
Packaging: 50mg
Price: $280
Updated: 2021/12/16

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BEPOTASTINE BESILATE Chemical Properties,Usage,Production

Description

Betotastine was introduced in Japan for the treatment of allergic rhinitis. This structurally-related derivative of chlorpheniramine and ebastine is prepared by condensation of optically-resolved 4-[1-(4-chlorophenyl)-1-(2-pyridyl)-methoxy]piperidine with ethyl 4-bromobutyrate followed by ester hydrolysis. Betotastine is the seventh marketed non-sedating histamine H₁ antagonist. Its very low sedative side effect is due to very poor penetration in the central nervous system. Besides its potent and long-acting activity in models of allergic rhinitis, betotastine was also shown to act as a PAF antagonist and inhibit LTD₄ in tracheal smooth muscle and ileum, IL-5 production by human peripheral blood mononuclear cells as well as eosinophil infiltration in the airway and peripheral blood. As a consequence, it is currently being developed against other allergic and respiratory disorders.

Description

Bepotastine is an antagonist of the histamine H₁ receptor that is selective over H₃, α₁-, α₂-, and β-adrenergic, dopamine D_2long, serotonin 5-HT₂, muscarinic acetylcholine, and benzodiazepine receptors. It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED₅₀ = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED₅₀ = 3.2 μg/kg). Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner. Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.

Chemical Properties

Off-White to Light Beige Solid

Originator

UBE (Japan)

Uses

Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7

Uses

Bepotastine is a histamine H1 receptor anatagonist. Bepotastine suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).

Definition

ChEBI: An organosulfonate salt obtained by combining equimolar amounts of bepotastine and benzenesulfonic acid. A topical, selective and non-sedating histamine (H1) receptor antagonist used for treatment of itching associated with allergic co junctivitis.

Manufacturing Process

Manufacturing process for BEPOTASTINE BESILATE includes these steps as follows: Step A: Synthesis of Methyl 2-endo-hydroxy-1-exo-hydroxymethyl-3a,8b-cis-2,3,3a,8b-tetrahydro- 1H-5-cyclopenta[b]benzofurancarboxylate,Step B: Synthesis of Methyl 3-methyl-trans-4a-cisoid-4a,5a-cis-5a-1,4a,5,5a,10b,10c-hexahydro-7- dioxin o[5,4-a]cyclopenta[b]benzofurancarboxylate,Step C: Synthesis of 3-Methyl-trans-4a-cosoid-4a,5a-cis-5a-1,4a,5,5a,10b,10c-hexahydro-7- dioxino[5,4-a]cyclopenta[b]benzofuranylmethanol,Step D: Synthesis of 7-Chloromethyl-3-methyl-trans-4a-cisoid-4a,5a-cis-5a-1,4a,5,5a,10b,10chexahydrodioxino[5,4-a]cyclopenta[b]benzofuran,Step E: Synthesis of 4-[3-Methyl-trans-4a-cisoid-4a,5a-cis-5a-1,4a,5,5a,10b,10c-hexahydro-7- dioxino[5,4-a]cyclopenta[b]benzofuranyl]butyric acid, Step F: Synthesis of Methyl 4-[2-endo-hydroxy-1-exo-hydroxymethyl-3a,8b-cis-2,3,3a,8btetrahydro-1H-5- cyclopenta[b]benzofuranyl]butyrate, Step G: Synthesis of Methyl 4-[2-endo-acetoxy-1-exo-hydroxymethyl-3a,8b-cis-2,3,3a,8btetrahydro-1H-5-cyclopenta[b]benzofuranyl]butyrate, Step H: Synthesis of Methyl ester of 11,15-dideoxy-11-acetoxy-16-methyl-15-oxo-18,19- tetradehydro-5,6,7-trinor-4,8-inter-m-phenylene PGI2,Step I: Synthesis of 11-Deoxy-11-acetoxy-16-methyl-18,19-tetradehydro-5,6,7-trinor-4,8-inter-mphenylene PGI2.To a solution of 54 mg of methyl ester of 11-deoxy-11-acetoxy-16-methyl- 18,19-tetradehydro-5,6,7-trinor-4,8-inter-m-phenylene PGI2 in 4.5 ml of anhydrous methanol was added 0.001 ml of 4.8 N sodium methoxide under argon, and the reaction mixture was stirred for 1.5 hours at room temperature. After addition of acetic acid to the reaction mixture and concentration of the mixture, the residue was dissolved in 20 ml of ethyl acetate, and the solution was washed with aqueous saturated solution of sodium hydrogen carbonate, water and aqueous saturated solution of sodium chloride, dried and concentrated to afford 55 mg of an oily material. This oily material was purified by column chromatography using ethyl acetate and cyclohexane (3:1) as eluent to give 48 mg of the methyl ester of 16- methyl-18,19-tetradehydro-5,6,7-trinor-4,8-inter-m-phenylene PGI2.

brand name

Talion

Therapeutic Function

Antiallergic

BEPOTASTINE BESILATE Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from BEPOTASTINE BESILATE manufacturers

Hebei Duling International Trade Co. LTD

Product: Bepotastine Besilate 190786-44-8
Price: US $50.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100 tons
Release date: 2023-04-19

WUHAN FORTUNA CHEMICAL CO., LTD

Product: Bepotastine besylate 190786-44-8
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 98.0%
Supply Ability: 1kg/month
Release date: 2021-09-26

Henan Bao Enluo International TradeCo.，LTD

Product: BEPOTASTINE BESILATE 190786-44-8
Price: US $30.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 1000tons
Release date: 2023-07-25

190786-44-8, BEPOTASTINE BESILATERelated Search:

sodium phenyl sulfate Isopropyl Benzenesulfonate Butyl Benzenesulfonate 2-hydroxyethyl benzenesulfonate Methyl benzenesulfonate Ramelteon 2-[(S)-(4-Chlorophenyl)(4-piperidinyloxy)methyl]pyridine (2R,3R)-2,3-Dihydroxybutanedioate 4-[(4-Chlorophenyl)-2-pyridinylmethoxy]-1-piperidinebutanoic acid Bepotastine Ethyl Ester 1-Piperidinebutanoic acid, 4-[(4-chlorophenyl)-2-pyridinylmethoxy]-, (R)- Fasudil hydrochloride FMOC-GLY-GLY-GLY-OH 5-alpha-Hydroxy- Laxogenin 5-[Bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazole-2-butanoic acid ethyl ester 1-Methyl-5-amino-1H-benzimidazole-2-butanoic acid ethyl ester ethyl 4-(1-methyl-5-nitro-1H-benzo[d]imidazol-2-yl)butanoate Benzenesulfonamide Ethyl benzenesulphonate

BEPOTASTINE BESILATE

(+)-(S)-4-(4-((4-Chlorophenyl)(2-pyridyl)methoxy)piperidino)butyric acid monobenzenesulfonate

4-((4-Chlorophenyl)-2-pyridinylmethoxy)- (S)-1-piperidinebutanoic acid monobenzenesulfonate

Talion (TN)

Bepotastine Beslilat

Bepotastine Besylate

1-Piperidinebutanoic acid, 4-[(4-chlorophenyl)-2-pyridinylmethoxy]-, (S)-, monobenzenesulfonate

1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-, monobenzenesulfonate

4-[4-[(R)-(4-chlorophenyl)-pyridin-2-yl-methoxy]-1-piperidyl]butanoic acid

(+)-(S)-4-[4-[1-(4-Chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid benzenesulfonate

Benzestatine

CS-645

CS-487

bepotastine benzenesulfonate salt

(S)-4-[4-(4-Chlorophenyl-2-pyridylMethoxy)piperidinyl]butyric Acid Benzenesulfonate

4-[(S)-(4-Chlorophenyl)-2-pyridinylMethoxy]-1-piperidinebutanoic Acid Benzenesulfonate

Bepotastine Benzenesulfonate

Bepreve

Talion

TAU 284

Bepotastine Beslilate

4-[4-[(4-chlorophenyl)-pyridin-2-ylMethoxy]piperidin-1-yl]butanoic acid benzenesulfonate

1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-, benzenesulfonate (1:1)

Benzenesulfonate salt

(S)-Bepotastine Besylate

Bepotastine Besilate (This product is only available in Japan.)

(S)-4-[4-[(4-Chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl]butanoic Acid Benzenesulfonate

4-[4-[(S)-(4-Chlorophenyl)(2-pyridinyl)methoxy]-1-piperidinyl]butanoic Acid Benzenesulfonate

BEPOTASTINE BESILATE USP/EP/BP

Betastine besylate

Bepotastine Besilate (Bepreve)

Bepotastine BesilateQ: What is Bepotastine Besilate Q: What is the CAS Number of Bepotastine Besilate Q: What is the storage condition of Bepotastine Besilate Q: What are the applications of Bepotastine Besilate

(S)-4-(4-((4-Chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid compound with benzenesulfonic acid (1:1)

(S)-4-(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid, benzenesulfonic acid

190786-44-8

C21H25ClN2O3C6H6O3S

C27H31ClN2O6S

54706

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