开发表皮生长因子受体抑制剂厄达非替尼的改进型简易合成路线

IF 1.8 3区化学 Q3 CHEMISTRY, ORGANIC Synthetic Communications Pub Date : 2024-11-05 DOI:10.1080/00397911.2024.2423897

Shuang Wang , Nanxin Peng , Liping Yin , Wei Wang , Yue Wu , Di Zhang , Zongjie Gan

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引用次数: 0

摘要

我们开发出了一种简便实用的厄达菲替尼合成路线。在这一路线中，关键中间体 N1-(3,5-二甲氧基苯基)-N2-异丙基乙烷-1,2-二胺（12）是通过一种新颖的两步法，从现成的凝视材料--3,5-二甲氧基苯胺（5）和 2-溴乙胺氢溴酸盐（16）制备的，总产率为 70%。随后，由化合物 12 和 7-溴-2-(1-甲基-1H-吡唑-4-基)喹喔啉（4）合成了 Erdafitinib，收率为 80%，纯度为 99%。这种替代方法为生产厄达非替尼提供了一条经济、高效的途径。

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Development of an improved and facile synthesis route of the FGFR inhibitor erdafitinib

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.

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来源期刊

Synthetic Communications 化学-有机化学

CiteScore

4.40

自引率

4.80%

发文量

156

审稿时长

4.3 months

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.