Bilastine | 202189-78-4

Bilastine Properties

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
FDA UNII	PA1123N395
ATC code	R06AX29

Pharmacokinetic data

Protein binding	84-90%
Excreted unchanged in urine	28.3%
Volume of distribution	1.29(L/kg)
Biological half-life	14.5 / -

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS07

Signal word

Warning

Hazard statements

H302

Precautionary statements

P280-P305+P351+P338

HS Code

2933.39.4100

NFPA 704

	0
3		0

Bilastine price More Price(34)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
TCI Chemical	B5392	Bilastine >98.0%(HPLC)(T)	202189-78-4	250mg	$104	2024-03-01	Buy
TCI Chemical	B5392	Bilastine >98.0%(HPLC)(T)	202189-78-4	1g	$286	2024-03-01	Buy
Cayman Chemical	28375	Bilastine	202189-78-4	25mg	$44	2024-03-01	Buy
Cayman Chemical	28375	Bilastine	202189-78-4	50mg	$84	2024-03-01	Buy
Cayman Chemical	28375	Bilastine	202189-78-4	100mg	$155	2024-03-01	Buy

Product number	Packaging	Price	Buy
B5392	250mg	$104	Buy
B5392	1g	$286	Buy
28375	25mg	$44	Buy
28375	50mg	$84	Buy
28375	100mg	$155	Buy

Bilastine Chemical Properties,Uses,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

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

Uses

Bilastine 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.

Synthesis_202189-78-4

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

Bilastine Suppliers

Global( 256)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	7613	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21695	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Hefei TNJ Chemical Industry Co.,Ltd.	+86-0551-65418679 +86-18949832763	info@tnjchem.com	China	2989	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Zhejiang ZETian Fine Chemicals Co. LTD	18957127338	stella@zetchem.com	China	2141	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58

Supplier	Advantage
Henan Fengda Chemical Co., Ltd	58
Capot Chemical Co.,Ltd.	60
Henan Tianfu Chemical Co.,Ltd.	55
ATK CHEMICAL COMPANY LIMITED	60
Hefei TNJ Chemical Industry Co.,Ltd.	55
career henan chemical co	58
Zhejiang ZETian Fine Chemicals Co. LTD	58
Biochempartner	58
Hubei Jusheng Technology Co.,Ltd.	58
BOC Sciences	58

View Lastest Price from Bilastine manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2024-03-26	Bilastine 202189-78-4	US $3.00-0.20 / KG	1KG	98%	g-kg-tons, free sample is available	Henan Fengda Chemical Co., Ltd
2024-01-04	Bilastine 202189-78-4	US $0.00-0.00 / kg	1kg	99%, Single impurity＜0.1	1 ton	Nanjing Fred Technology Co., Ltd
2023-04-04	bilastine 202189-78-4	US $0.00-0.00 / ml	1ml	98%	1000L per month	Zhejiang Hengkang Pharmaceutical Co., Ltd.

Bilastine
202189-78-4
US $3.00-0.20 / KG
98%
Henan Fengda Chemical Co., Ltd

Bilastine
202189-78-4
US $0.00-0.00 / kg
99%, Single impurity＜0.1
Nanjing Fred Technology Co., Ltd

bilastine
202189-78-4
US $0.00-0.00 / ml
98%
Zhejiang Hengkang Pharmaceutical Co., Ltd.

Bilastine Spectrum

BENZENEACETIC ACID, 4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL)-1-PIPERIDINYL)ETHYL-ALPHA, ALPHA-DIMETHYL-(202189-78-4)¹HNMR

202189-78-4(Bilastine)Related 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

1of4

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 Bilasten 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 2-[4-[2-[4-[1-(2-Ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylproionic acid Bilatex 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)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 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 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 Bilastine Bilastin Bilaxten 2-(4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZO[D ]IMIDAZOL-2-YL) PIPERIDIN-1-YL)ETHY)PHEN YL)-2-METHYLPROPANOIC ACID Bilastine (Form-I) 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoicaci Bilastine In-House Bilastene 202189-78-4 C28H31D6N3O3 Aromatics Heterocycles Intermediates & Fine Chemicals Pharmaceuticals Isotope Labelled Compounds API