Shuang Wang , Nanxin Peng , Liping Yin , Wei Wang , Yue Wu , Di Zhang , Zongjie Gan
{"title":"Development of an improved and facile synthesis route of the FGFR inhibitor erdafitinib","authors":"Shuang Wang , Nanxin Peng , Liping Yin , Wei Wang , Yue Wu , Di Zhang , Zongjie Gan","doi":"10.1080/00397911.2024.2423897","DOIUrl":null,"url":null,"abstract":"<div><div>A facile and practical synthetic route for erdafitinib has been developed. In this route, the key intermediate <em>N<sup>1</sup></em>-(3,5-dimethoxyphenyl)-<em>N<sup>2</sup></em>-isopropylethane-1,2-diamine (<strong>12</strong>) was prepared from readily available staring materials, 3,5-dimethoxyaniline (<strong>5</strong>) and 2-bromoethylamine hydrobromide (<strong>16</strong>), through a novel two-step process with an overall yield of 70%. Erdafitinib was subsequently synthesized from compound <strong>12</strong> and 7-bromo-2-(1-methyl-1H-pyrazol-4-yl)quinoxaline (<strong>4</strong>) in 80% yield and 99% purity. This alternative procedure offers an economical and efficient route to produce erdafitinib.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 24","pages":"Pages 2120-2129"},"PeriodicalIF":1.8000,"publicationDate":"2024-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Synthetic Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S0039791124001292","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
引用次数: 0
Abstract
A facile and practical synthetic route for erdafitinib has been developed. In this route, the key intermediate N1-(3,5-dimethoxyphenyl)-N2-isopropylethane-1,2-diamine (12) was prepared from readily available staring materials, 3,5-dimethoxyaniline (5) and 2-bromoethylamine hydrobromide (16), through a novel two-step process with an overall yield of 70%. Erdafitinib was subsequently synthesized from compound 12 and 7-bromo-2-(1-methyl-1H-pyrazol-4-yl)quinoxaline (4) in 80% yield and 99% purity. This alternative procedure offers an economical and efficient route to produce erdafitinib.
期刊介绍：
Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.
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