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| Process Improvement on the Synthesis of Halofuginone Intermediate |
| WANG Chao-jie, WAN Yang, SONG Wei-qiang, LU Qun |
| School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China |
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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.
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Received: 14 January 2015
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2016, Vol. 24 
