1181267-32-2Relevant articles and documents
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.
PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS
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Page/Page column 5, (2011/02/15)
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