芳构化
酮洛芬
化学
部分
热解炭
非甾体
三氟甲磺酸
组合化学
羟醛反应
产量(工程)
有机化学
催化作用
药理学
热解
材料科学
医学
冶金
色谱法
作者
Lili Song,Zhigang Liu,Lei Zhu,Pei Tang,Fen‐Er Chen
标识
DOI:10.1021/acs.oprd.3c00049
摘要
The practical synthesis of the representative nonsteroidal anti-inflammatory drug ketoprofen has been accomplished in 44% overall yield on the decagram scale. The key features in this synthetic work involve a TiCl4–Et3N mediated aldol/enol-lactonization annulation to affect dihydrobenzofuranone core formation and the use of a highly efficient pyrolytic aromatization condition to facilitate the construction of the vital 2-arylpropionic acid (2-APA) moiety. Furthermore, the avoidance of hazardous chemicals and crystallization of several intermediates would be greatly beneficial to the scalable synthesis of ketoprofen.
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