32454-35-6Relevant articles and documents
Palladium-Catalyzed Distal m-C-H Functionalization of Arylacetic Acid Derivatives
Srinivas, Dasari,Satyanarayana, Gedu
supporting information, p. 7353 - 7358 (2021/10/01)
Herein, we present m-C-H olefination on derivatives of phenylacetic acids by tethering with a simple nitrile-based template through palladium catalysis. Notably, the versatility of the method is evaluated with a wide range of phenylacetic acid derivatives for obtaining the meta-olefination products in fair to excellent yields with outstanding selectivities under mild conditions. Significantly, the present strategy is successfully exemplified for the synthesis of drugs/natural product analogues (naproxen, ibuprofen, paracetamol, and cholesterol).
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.
A α - (4 - substituted phenyl) of isobutyric acid preparation method
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Paragraph 0076, (2017/08/26)
The invention relates to the field of organic chemical synthesis and discloses a preparation method of alpha-(4-substituted phenyl)isobutyric acid. The method comprises the steps of respectively carrying out Friedel-Crafts acylation, condensation reaction, rearrangement reaction and hydrolytic acidification reaction on single substituted benzene and 2-haloisobutyryl halide or isobutyryl halide serving as an acylating agent to finally prepare a finished product of alpha-(4-substituted phenyl)isobutyric acid. The preparation method provided by the invention has the advantages that the raw materials are easily obtained and are relatively low in toxicity, a catalysis system of the rearrangement reaction can effectively promote the rearrangement reaction, the obtained product is relatively high in purity and yield, the whole preparation method is simple, the adopted reagent is safe, and the preparation method is beneficial to industrial production.