A facile and efficient method for the synthesis of N-substituted isoindolin-1-one derivatives under Pd(OAc)(2)/HCOOH system

作者：Zhou, Yang; Chen, Ping; Lv, Xue; Niu, Junxing; Wang, Yingying; Lei, Min^*; Hu, Lihong^*

来源：Tetrahedron Letters, 2017, 58(23): 2232-2235.

DOI：10.1016/j.tetlet.2017.04.073

• 2-Formylbenzoic acid
• Isoindolin-1-one
• Pd(OAc)(2)
• Hydrogenation
• Cyclization

A facile and efficient method for the synthesis of N-substituted isoindolin-1-one derivatives from 2-formylbenzoic acid and amine under Pd(OAc)(2)/HCOOH system has been described. The whole process is carried out in ligand-free conditions and furnished the desired products by reductive intramolecular cyclization. Furthermore, this procedure is applied successfully for the modification of natural products, such as vindoline and estrone.

• 出版日期2017-6-7
• 单位中国科学院上海药物研究所; 中国科学院大学; 武汉轻工大学; 南京中医药大学