提高依度沙班中间体合成产率的探究  

Exploration on Improving the Synthesis Yield of Edoxaban Intermediates

作　　者：徐瑾 漆定超 Xu Jin;Qi Dingchao(Cangzhou Narui Chemical Technology Co.,Ltd.,Hebei,061000)

机构地区：[1]沧州那瑞化学科技有限公司,河北061000

出　　处：《当代化工研究》2024年第6期174-176,共3页Modern Chemical Research

摘　　要：依度沙班是重要的药物中间体,但其中间体的合成一直面临收率低的难题。本文在综述现有合成方法的基础上,采用自主设计的铁氧体催化剂,并优化反应条件,实现了依度沙班中间体收率的大幅提高。首先,文章比较了苯酚法、环氧氯丙烷法和马来酐法等合成途径的优劣。其次,讨论了温度、催化剂、溶剂等因素对收率的影响,提出了催化剂和反应条件优化设想。采用新设计的铁氧体催化剂,转换率可达83.2%。进一步优化反应条件后,收率可达92.3%。本研究取得的重要进展,为依度沙班中间体的工业生产提供了简便、高效的新合成方法。Edoxaban is an important pharmaceutical intermediate,but the synthesis of its intermediate has always faced the challenge of low yield.On the basis of reviewing existing synthesis methods,this article adopts self-designed ferrite catalysts and optimizes reaction conditions,achieving a significant increase in the yield of Edoxaban intermediate.Firstly,the article compared the advantages and disadvantages of synthesis methods such as phenol method,epichlorohydrin method,and maleic anhydride method.Secondly,the effects of temperature,catalyst,solvent and other factors on the yield were discussed,and ideas for optimizing the catalyst and reaction conditions were proposed.Using a newly designed ferrite catalyst,the conversion rate can reach 83.2%.After further optimizing the reaction conditions,the yield can reach 92.3%.This study has made sig-nificant progress and provided a simple and efficient new synthesis method for the industrial production of Edoxaban intermediates.

关 键 词：依度沙班 中间体合成 提高 

分 类 号：TQ[化学工程]