当前位置: X-MOL 学术Helv. Chimica Acta › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Improvements in the Synthesis of the Third-Generation EGFR Inhibitor Osimertinib
Helvetica Chimica Acta ( IF 1.8 ) Pub Date : 2021-09-12 , DOI: 10.1002/hlca.202100066
Konstantinos Skobridis 1 , Pinelopi Voulgari 2 , Dimitrios Alivertis 3
Affiliation  

Osimertinib, a third generation potent and specific EGFR inhibitor is an important drug against many forms of cancer. It was synthesized by an improved and highly efficient protocol, revisiting the classical synthetic process and modifying parameters, such as solvents, temperature, reagents, and reaction time. A cost-effective, environmentally friendly methodology for the synthesis of osimertinib was established, which gave shorter reaction times, saved labor by eliminating purification steps through column chromatography, and enhanced yields. Four of the seven steps in total, were proceeded quantitatively or almost quantitatively (ca. 98 %). This synthetic protocol provides a very high overall yield, up to 68 %. In addition, the entire approach enables the preparation of osimertinib analogues and could be extended in the synthesis of other structurally similar bioactive compounds.

中文翻译:

第三代EGFR抑制剂奥希替尼合成的改进

奥希替尼是第三代强效特异性 EGFR 抑制剂,是对抗多种癌症的重要药物。它是通过改进的高效方案合成的,重新审视经典的合成过程并修改了溶剂、温度、试剂和反应时间等参数。建立了一种经济高效、环境友好的奥希替尼合成方法,该方法缩短了反应时间,通过消除柱层析纯化步骤节省了劳动力,并提高了产量。总共七个步骤中的四个是定量或几乎定量进行的(大约. 98%)。该合成方案提供了非常高的总产率,高达 68%。此外,整个方法能够制备奥希替尼类似物,并且可以扩展到其他结构相似的生物活性化合物的合成中。
更新日期:2021-11-15
down
wechat
bug