1181267-38-8Relevant articles and documents
Preparation method of bilastine key intermediate
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Paragraph 0036-0039; 0042-0095, (2021/08/25)
The invention belongs to the technical field of drug synthesis, and relates to 2 - (4 - (2 - (4 -ethoxyethyl) 1 - benzo [2 -] imidazol - 1H - yl) piperi d-ethyl) phenyl) -2 -methylpropionate (-1 -), and a -2 - complex and II acid are used as a catalyst to condensation the enolate anion with the compound (16 15) to form a target product II Ni Lewis. The invention aims to provide a short synthetic route. The provided route raw material condition is mild, the yield is high, the tedious building quaternary carbon atom method reported in the traditional process is avoided, and the method is suitable for industrial production.
Preparation method of bilastine
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Paragraph 0077; 0078, (2020/04/17)
The invention provides a preparation method of bilastine. Specifically the method comprises the following steps: oxidizing 4-hydroxyethyl phenyl methyl tert-butyrate to obtain 4-acetaldehyde phenyl methyl tert-butyrate, and carrying out a reductive aminat
A new and competitive synthetic approach for an antihistamine agent, bilastine
Kommera, Rajashekar,Yerrabelly, Jayaprakash Rao,Kasireddy, Venkateshwarreddy,Ghojala, Venkat Reddy,Singavarapu, Adilakshmi,Rebelli, Pradeep
, p. 815 - 821 (2018/11/06)
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.