API and Intermediate

bilastine

Product Name:Bilastine
Synonyms:Bilatex;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;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-;Bilasten
CAS:202189-78-4
MF:C28H37N3O3
MW:463.61 
Product Categories:Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds
Type:Pharmaceutical Intermediates
Appearance:White powder
Purity:99%
Package:5G;10G;25G;50G;100G;250G;1KG
Applications:Bilastine is a second-generation antihistamine medication which is used in the treatment of allergic rhinoconjunctivitis and urticaria.
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.

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