Yield:865471-20-1 79.6%

Reaction Conditions:

in 1,4-dioxane;Reflux;

Steps:

4.1.9. The general procedures for the preparation of intermediates24a-f

General procedure: To the solutions of various 2-fluorobenzoic acids 23ad(2.7 mmol) in 20 mL dioxane, morpholine (1.2 mL, 13.5 mmol) orpiperidine (1.1 mL, 13.5 mmol) was added in one potion. The reactionswere stirred at refluxing temperature, after the reactionscompleted, solvents and remaining morpholine or piperidine wereremoved in vacuo. Then, the residues were dissolved intowater andneutralized by 10% HCl aqueous. The resulting precipitate werecollected, washed by water, and dried to give intermediates 24a-f.

References:

Zhu, Huajian;Li, Wenlong;Shuai, Wen;Liu, Yang;Yang, Limei;Tan, Yuchen;Zheng, Tiandong;Yao, Hong;Xu, Jinyi;Zhu, Zheying;Yang, Dong-Hua;Chen, Zhe-Sheng;Xu, Shengtao [European Journal of Medicinal Chemistry,2021,vol. 216,art. no. 113316]