Zhang Xiaopeng, Pang Qiuyang, Liu Dan, Guo Zhenhua, Zhang Guisheng
NMPA Key Laboratory for Research and Evaluation of Innovative Drug, Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007, People's Republic of China.
Org Biomol Chem. 2024 Apr 3;22(14):2791-2796. doi: 10.1039/d4ob00055b.
A facile and direct approach to 1-substituted 2,3-dihydroquinazolin-4(1)-ones has been developed Pd(II)-catalyzed one-pot cascade annulation of -substituted anilines with CO, NHOAc and aldehydes, and it features an intrinsic directing strategy, cheap and easily obtainable raw materials, low cost, high step economy and efficiency, broad substrate scope and good product diversity. This protocol has been successfully applied to the synthesis of glycozolone A and gram-level experiments. Based on the control experiments and the literature, the reaction mechanism was proposed.
已开发出一种简便直接的方法来合成1-取代的2,3-二氢喹唑啉-4(1)-酮，即通过钯(II)催化的α-取代苯胺与CO、NHOAc和醛的一锅串联环化反应，该方法具有内在导向策略、原料廉价易得、成本低、步骤经济性和效率高、底物范围广以及产物多样性好等特点。该方案已成功应用于糖唑酮A的合成及克级实验。基于对照实验和文献，提出了反应机理。
