Wang Kai, Ouyang Jun, Liu Huan, Yin Lijun, Yang Kuoqi, Lan Lefu, Hu Youhong, Hu Naifu
Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, 1 Sub-lane Xiangshan, Hangzhou 310024, P.R. China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No. 555, Zuchongzhi Road, Pudong, Shanghai 201203, P.R. China.
J Org Chem. 2024 Dec 20;89(24):18746-18751. doi: 10.1021/acs.joc.4c02443. Epub 2024 Dec 10.
A novel method is reported to synthesize various pyrazolones through transition-metal-free and redox-neutral 1°, 2°, or 3° C(sp)-H carbonylative cyclization using 1 atm of CO as a green carbonyl source, featuring good functional group tolerance, a broad substrate scope, facile scalability, and easy product transformation. The utility of this method could be demonstrated by the applications in preparing useful synthetic intermediates and bioactive compounds.
据报道，一种新方法可通过使用1个大气压的CO作为绿色羰基源，进行无过渡金属和氧化还原中性的一级、二级或三级C(sp)-H羰基化环化反应来合成各种吡唑啉酮，该方法具有良好的官能团耐受性、广泛的底物范围、易于放大以及产物易于转化的特点。该方法的实用性可通过其在制备有用的合成中间体和生物活性化合物中的应用得到证明。
