Study On The Process Of Febuxostat And Its A Crystals

Febuxostat is a new generation of anti-gout drugs synthesized by Teijin PHarma,Japan,and is the first anti-gout drug approved by the Food and Drug Administration for nearly 40 years.It is a selective xanthine oxidase/xanthine dehydrogenase inhibitor,showing excellent activity,less adverse reactions.In 2012 American College of Rheumatology gout guidelines will be febuxostat as a recommendation of A-class drugs.Febuxostat is a very important anti-gout drugs,has a good development prospects.This paper aims to study the improvement of the synthesis process of the treatment of associated gout with hyperuricemia drugs febuxostat and its relatively stable crystalline A crystals.First of all,on the basis of in reference to a large number of literature and the actual production conditions,through the febuxostat process to summarized and compared.Then,cheap p-hydroxythiobenzamide was selected as the starting material,febuxostat was obtained by cyclization,Duff reaction,etherification,cyanidation and hydrolysis.Finally,febuxostat A crystal is obtained by crystal transformation.The process route reaction conditions mild step,easy to operate.The reaction conditions of each step were optimized to determine the preparation process of febuxostat and A crystal;Through the analysis of elemental composition,IR,1H-NMR,13C-NMR,MS and X-ray diffraction spectra,the product Structure consistent with febuxostat and A crystal molecular characteristics;At the same time enlarge production also proved that the process is feasible,suitable for industrial production.