1181267-32-2

Upstream product

• 1000536-33-3 2-methyl-2-(4-(2-hydroxyethyl)phenyl)propionic acid methyl ester 
• 124-63-0 methanesulfonyl chloride 
• 154825-97-5 methyl 2-(4-bromophenyl)-2,2-dimethylacetate 

Downstream Products

• 1181267-37-7 2-(4-{2-[4-(1H-benzoimidazol-2-yl)-piperidin-1-yl]-ethyl}phenyl)-2-methyl-propionic acid methyl ester 
• 1181267-38-8 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidine]ethyl]-α,α-dimethylphenylacetic acid methyl ester 
• 202189-78-4 Bilastine 

Relevant academic research and scientific papers

A new and competitive synthetic approach for an antihistamine agent, bilastine

Efforts towards the novel synthesis of second generation non-sedating antihistamine drug, Bilastine was described in this manuscript. This competitive synthetic approach involves the convergent synthesis of Bilastine via simple Friedel-Crafts acylation as an alternate for earlier reported Stille and Suzuki couplings. The selectivity in Friedel-Crafts acylation reaction with chloro acetyl chloride on different substituted arenes was studied and employed the best conditions for the synthesis of Bilastine. Further synthetic approach involves the deoxygenation of aryl ketone to corresponding alkane in single step and finally provides Bilastine with 39% of improved overall yields, utilizing simple and cost-effective reagents, suitable for kilogram scale synthesis.

PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS

The present invention relates to a process for preparing 2-methyl-2′-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present inv

Alternative synthesis of bilastine

A new and efficient synthesis of the non-sedating histamine H1 receptor antagonist Bilastine is reported. The new route employs a convergent strategy, with a longest linear sequence of five steps, giving slightly improved yields over the previous routes.

PROCESS FOR PREPARATION OF 2-METHYL-2′-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS

The present invention relates to a process for preparing 2-methyl-2'-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present inv