Zhang Jingyi, Li Ying, Zhang Chaofeng, Wang Xiao-Na, Chang Junbiao
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, P. R. China.
Org Lett. 2021 Mar 19;23(6):2029-2035. doi: 10.1021/acs.orglett.1c00158. Epub 2021 Mar 1.
A novel metal-free [3+2] annulation of ynamides with anthranils provides a facile, flexible, environmentally friendly, and atom-economical route to 2-aminoindoles. This synthetic process proceeds with efficiency, excellent regioselectivity, and wide functional group tolerance under mild conditions. Moreover, the obtained 2-aminoindole products represent a multifunctional platform for the construction of various 2-aminoindolyl frameworks.
一种新型的炔酰胺与邻氨基苯甲酰亚胺的无金属[3+2]环化反应为合成2-氨基吲哚提供了一条简便、灵活、环境友好且原子经济的途径。该合成过程在温和条件下高效进行，具有出色的区域选择性和广泛的官能团耐受性。此外，所得到的2-氨基吲哚产物是构建各种2-氨基吲哚基骨架的多功能平台。
