朱建明 (厦门迈克制药有限公司 福建厦门 361022)
摘 要 目的：优化帕珠沙星Hofmann重排反应的合成工艺。方法：按L9(34)正交表设计考察帕珠沙星Hofmann重排反应影响因素，并对反应时间(A)、反应温度(B)、次氯酸钠的浓度(C)、次氯酸钠的用量（D）4个主要因素进行优选，每个因素各取3个水平。结果：合成帕珠沙星的Hofmann重排反应最优反应条件为A1 B1 C2 D2，收率可达70.5%。结论：最佳工艺参数简单易控制，提高了收率，适合工业化生产。
关键词 正交设计; 帕珠沙星; Hofmann重排
中图分类号：R914.5
文献标识码：A
文章编号：1008-049X(2007)03-0249-02
Optimization of Hofmann Rearrangement of Pazufloxacin by Orthogonal Design
Zhu Jianming (Xiamen Mchem Laboratories LTD, Fujian Xiamen 361022,China)
ABSTRACT Objective: To optimize the process of Hofmann rearrangement of pazufloxacin.Method: Target compound pazufloxacin was synthesized through the Hofmann rearrangement reaction. Four main factors were influenced yield of synthesis pazufloxacin, such as reaction time(A), reaction temperature(B),concentration of sodium hypochlorite (C),quantity of sodium hypochlorite(D),each being selected three levels，were evaluated by the orthogonal experimental design of L9(34).Result: The optimization terms of the Hofmann rearrangement were A1B1C2D2.The yield of pazufloxacin reached 70%. Conclusion: The process parameters are simple and easy to control. The yield of pazufloxacin is improved. The process is suitable for industrial production.
KEY WORDS Orthogonal design；Pazufloxacin；Hofmann rearrangement
作者简介：朱建明，男，高级工程师，主要从事化学药物合成研究。
Tel: (0592)6518598
E-mail: laoming0592@hotmail.com
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