Abstract:Halofuginone intermediate, 1-(3-methoxypiperidin-2-yl)propan-2-one, was synthesized by ring-expansion, methylation, deprotonation, nucleophilic addition, ketalation, hydrogenation and hydrolysis, using 2-acetylfuran as the starting material. The overall yield was 40.2%. The structure was confirmed by 1H NMR and ESI-MS.
王超杰, 万阳, 宋卫强, 陆群. 常山酮中间体的合成工艺改进[J]. 合成化学, 2016, 24(1): 79-83.
WANG Chao-jie, WAN Yang, SONG Wei-qiang, LU Qun. Process Improvement on the Synthesis of Halofuginone Intermediate. Chinese Journal of Synthetic Chemistry, 2016, 24(1): 79-83.