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| 氟苯尼考的合成工艺研究 | |
| 引用本文： | 吴春丽,王胜强,丁书超,张桥. 氟苯尼考的合成工艺研究[J]. 中国药物化学杂志, 2007, 17(3): 160-162 |
| 作者姓名： | 吴春丽 王胜强 丁书超 张桥 |
| 作者单位： | 1. 郑州大学,药学院,河南,郑州,450052;郑州大学,新药研发中心,河南,郑州,450052 2. 郑州大学,新药研发中心,河南,郑州,450052 3. 郑州华伦生物技术有限公司,河南,郑州,450001 4. 郑州大学,药学院,河南,郑州,450052 |
| 摘 要： | 目的研究氟苯尼考的合成工艺。方法以（1R,2R）-3-羟基-2-氨基-3-[4-（甲砜基）苯基]-丙酸乙酯为原料,经过还原、保护、氟化、水解、二氯乙酰化5步反应最后得到氟苯尼考。结果与结论该合成路线简单,原料易得,目标化合物的总收率为78%。 |
| 关 键 词： | 工艺研究 氟苯尼考 N,N-二乙基-(1,1,2,3,3,3-六氟丙基)-胺 |
| 文章编号： | 1005-0108（2007）03-0160-03 |
| 收稿时间： | 2006-11-08 |
| 修稿时间： | 2006-11-08 |
Improved synthesis of florfenicol |
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| WU Chun-li,WANG Sheng-qiang,DING Shu-chao,ZHANG Qiao. Improved synthesis of florfenicol[J]. Chinese Journal of Medicinal Chemistry, 2007, 17(3): 160-162 | |
| Authors: | WU Chun-li WANG Sheng-qiang DING Shu-chao ZHANG Qiao |
| Affiliation: | 1. Pharmaceutical College of Zhengzhou University, Zhengzhou 450052, China ; 2. Pharmaceutical College of Zhengzhou University, New Drug Research-development Centre, Zhengzhou 450052, China ; 3. Zhengzhou Heallen Bio-tech Co. Ltd., Zhengzhou 450001, China |
| Abstract: | Aim To improve a synthetic route of florfenicol.Methods The target compound was synthesized by using(1R,2R)-3-hydroxy-2-amino3-[4-(methylsulfonyl)-phenyl]-ethyl propionate as starting material,via a five steps process including reduction,protection,fluorination,hydrolyzation,dichloroacetylation.Results and conclusion The starting materials in the synthetic route are easily available and the total yield is 78%.The synthetic procedure of intermediates 3-6 were improved. |
| Keywords: | process research florfenicol FPA |
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