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Bilastine

Product Name
Bilastine
CAS No.
202189-78-4
Chemical Name
Bilastine
Synonyms
Bilastine;Bilastin;2-(4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZO[D ]IMIDAZOL-2-YL) PIPERIDIN-1-YL)ETHY)PHEN YL)-2-METHYLPROPANOIC ACID;Bilaxten;Bilatex;Bilasten;Bilastene;Bilastine -IP/BP/;Bilastine (Form-I);Bilastine In-House
CBNumber
CB81011081
Molecular Formula
C28H37N3O3
Formula Weight
463.62
MOL File
202189-78-4.mol
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Bilastine Property

Melting point:
202 °C
Boiling point:
639.1±55.0 °C(Predicted)
Density 
1.16±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,Room Temperature
Water Solubility 
Insoluble in water
solubility 
DMSO:49.3(Max Conc. mg/mL);106.34(Max Conc. mM)
pka
4.40±0.10(Predicted)
form 
powder to crystal
color 
White to Light yellow
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Safety

HS Code 
2933.39.4100
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

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

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

TCI Chemical
Product number
B5392
Product name
Bilastine
Purity
>98.0%(HPLC)(T)
Packaging
250mg
Price
$104
Updated
2024/03/01
TCI Chemical
Product number
B5392
Product name
Bilastine
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$286
Updated
2024/03/01
Cayman Chemical
Product number
28375
Product name
Bilastine
Packaging
25mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
28375
Product name
Bilastine
Packaging
50mg
Price
$84
Updated
2024/03/01
Cayman Chemical
Product number
28375
Product name
Bilastine
Packaging
100mg
Price
$155
Updated
2024/03/01
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Bilastine Chemical Properties,Usage,Production

Description

Bilastine, a potent and selective histamine H1 receptor antagonist, was approved in Europe in 2010 for the treatment of allergic rhinoconjunctivitis (AR) and urticaria (hives or skin rash). The original synthesis of bilastine involves alkylation of 2-piperidinyl-1H-benzimidazole with a phenethyltosylate, the para position of which is substituted with a dimethyloxazoline moiety serving as a masked carboxylic acid group. Alkylation of the benzimidazole nitrogen with 2-chloroethyl ethyl ether followed by unmasking of the oxazoline moiety with sulfuric acid provided bilastine.
In two major clinical trials, bilastine was effective at relieving allergic rhinitis as assessed by measuring the severity of nasal (obstruction, rhinorrhea, itching, sneezing) and nonnasal (ocular itching, tearing, ocular redness, itching of ears, and/or palate) symptoms.

Description

Bilastine is a histamine H1 receptor antagonist (IC50 = 180 nM). It is selective for the histamine H1 receptor in a panel of 30 receptors in vitro at 100 μM. Bilastine prevents microvascular extravasation (ED50 = 185 μg/kg, i.v.), bronchospasm (ED50 = 4.6 μg/kg, i.v.), and systemic anaphylaxis (ED50 = 0.2 μg/kg, p.o.) induced by subcutaneous histamine in guinea pigs. It prevents anaphylaxis induced by subcutaneous administration of ovalbumin or dinitrophenylated human albumin (DNP) in sensitized rats when administered at doses of 7.6 and 6.0 mg/kg, respectively. Formulations containing bilastine have been used in the treatment of urticaria and allergic rhinitis.

Originator

FAES FARMA, S.A. (Spain)

Uses

Bilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

Uses

Labelled Bilastine. It is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

Definition

ChEBI: Bilastine is a member of benzimidazoles.

brand name

Bilaxten

Clinical Use

Bilastine is a selective histamine H1 antagonist approved for the treatment of allergic rhinoconjunctivitis and urticaria (hives). This drug, which has proven to be well tolerated in toxicology profiling, 46 was discovered by the Spainsh firm FAES Farma and was approved by the European Union in 2010.

Synthesis

In 2011, Collier and co-workers published a communication describing both the original synthesis of bilastine and an improved route which was amenable to gram-scale production. Collier?ˉs second generation route, shown below, relies upon a convergent approach involving the union of piperidinyl benzimidazole 49 with fully functionalized phenethyl electrophile 48.Coupling the commercially available bromophenyl acetate 44 with cyclic trioxatriborinane 45 under conventional Suzuki conditions furnished styrene 46 in good yield. Alternatively, this vinylation reaction was also performed under Stille conditions with tributyl vinyl stannane in 83% yield. Hydroboration¨Coxidation of 46 delivered phenethyl alcohol 47 which was then immediately mesylated under basic conditions in toluene to produce adduct 48. This sulfonate was then reacted with piperidine 49 (whose preparation is described in Scheme 7) followed by saponification of the resulting ester 50 to arrive at bilastene (VI) in 26% overall yield from 44.



For the preparation of bilastine piperidine 49, commercially available piperidine 51 was first protected as the Boc-carbamate 52 prior to alkylation of the benzimidazole nitrogen atom with 1-chloro-2-ethoxyethane 53, providing compound 54. The Boc group of 54 was removed under acidic conditions to give fragment 49. This sequence produced the desired piperidine component in 86% overall yield from 51.

Drug interactions

Potentially hazardous interactions with other drugs
Antivirals: concentration possibly increased by ritonavir.
Grapefruit juice: concentration of bilastine reduced.

Metabolism

Not significantly metabolised. Almost 95% of the administered dose was recovered in urine (28.3%) and faeces (66.5%) as unchanged bilastine

Bilastine Preparation Products And Raw materials

Raw materials

Preparation Products

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Bilastine Suppliers

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View Lastest Price from Bilastine manufacturers

Nanjing Fred Technology Co., Ltd
Product
Bilastine 202189-78-4
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%, Single impurity＜0.1
Supply Ability
1 ton
Release date
2024-01-03
Henan Fengda Chemical Co., Ltd
Product
Bilastine 202189-78-4
Price
US $3.00-0.20/KG
Min. Order
1KG
Purity
98%
Supply Ability
g-kg-tons, free sample is available
Release date
2024-03-26
Hebei Mojin Biotechnology Co., Ltd
Product
Bilastine 202189-78-4
Price
US $50.00/KG
Min. Order
10KG
Purity
99%
Supply Ability
1000kg
Release date
2020-06-30

202189-78-4, BilastineRelated Search:

Olopatadine Loratadine ORYZANOL Bilastine N-Oxide 1'-Hydroxy Bilastine tert-butyl 4-(1H-benzo[d]iMidazol-2-yl)piperidine-1-carboxylate 1-Naphthaleneacetic acid Pirenoxine Benzeneethanol, 4-[1-(4,5-dihydro-4,4-dimethyl-2-oxazolyl)-1-methylethyl]-, 4-methylbenzenesulfonate (ester) 2-(2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)propan-2-yl)-4,4-dimethyl-4,5-dihydrooxazole 2-Propenoic acid, 3-[3-[(phenylaMino)sulfonyl]phenyl]-, Methyl ester, (2E)- 4-FORMYLCINNAMIC ACID METHYL ESTER 2-Propenoic acid, 3-[3-[(phenylaMino)sulfonyl]phenyl]-, ethyl ester, (2E)- 2-(1-(4-(2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)propan- 2-yl)phenethyl)piperidin-4-yl)-1H-benzo[d]imidazole 4-[1-(4,5-DIHYDRO-4,4-DIMETHYL-2-OXAZOLYL)-1-METHYLETHYL]-BENZENEETHANOL [4-(2-AMINO-ETHYL)-PHENYL]-ACETIC ACID alinastine Bilastine

  • Bilastin
  • 4-[2-[4-[1-(2-Ethoxyethyl)-1H-benziMidazol-2-yl]-1-piperidinyl]ethyl]-α,α-diMethylbenzeneacetic Acid
  • Benzeneacetic acid,4-[2-[4-[1-(2-ethoxyethyl)-1H-benziMidazol-2-yl]-1-piperidinyl]ethyl]-a,a-diMethyl-
  • BENZENEACETIC ACID, 4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL)-1-PIPERIDINYL)ETHYL-ALPHA, ALPHA-DIMETHYL-
  • 2-[4-[2-[4-[1-(2-ethoxyethyl)benzoimidazol-2-yl]-1-piperidyl]ethyl]phenyl]-2-methyl-propanoic acid
  • 4-[2-[4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-alpha,alpha-dimethylbenzeneacetic acid
  • Bilastine
  • 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
  • the impurity of Bilastine
  • 2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
  • Bilasten
  • 2-[4-[2-[4-[1-(2-Ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylproionic acid
  • Bilatex
  • Bilaxten
  • Benzeneacetic acid, 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl-
  • BENZENEACETIC ACID, 4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL)-1-PIPERIDINYL)ETHYL-ALPHA, ALPHA-DIMETHYL- USP/EP/BP
  • 2-(4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZO[D ]IMIDAZOL-2-YL) PIPERIDIN-1-YL)ETHY)PHEN YL)-2-METHYLPROPANOIC ACID
  • 2-[4-[2-[4-[1-(2-Ethoxyethyl)benzimidazol-2-yl]piperidin-1-y...
  • 2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-3-methylpropanoic acid
  • Bilastine D6Q: What is Bilastine D6 Q: What is the CAS Number of Bilastine D6 Q: What is the storage condition of Bilastine D6 Q: What are the applications of Bilastine D6
  • BilastineQ: What is Bilastine Q: What is the CAS Number of Bilastine Q: What is the storage condition of Bilastine Q: What are the applications of Bilastine
  • Bilastine (Form-I)
  • 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoicaci
  • Bilastine In-House
  • Bilastene
  • Bilastine -IP/BP/
  • 202189-78-4
  • C28H31D6N3O3
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Isotope Labelled Compounds
  • API