[1]王溥照,何世波,詹一丰,等. 5-氟尿嘧啶-1-乙酰氯的合成工艺研究[J].湖北工业大学学报,2023,(1):59-61.
　WANG Puzhao,HE Shibo,ZHAN Yifeng,et al. Study on Synthesis Technology of 5-Fluorouracil-1-Acetyl Chloride[J].,2023,(1):59-61.
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 5-氟尿嘧啶-1-乙酰氯的合成工艺研究()
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《湖北工业大学学报》[ISSN:1003-4684/CN:42-1752/Z]

卷:
期数:
2023年第1期
页码:
59-61
栏目:
湖北工业大学学报
出版日期:
2023-03-13

文章信息/Info

Title:
 Study on Synthesis Technology of 5-Fluorouracil-1-Acetyl Chloride
文章编号:
1003-4684(2023)01-0059-03
作者:
 王溥照;  何世波;  詹一丰;  刘明星
 湖北工业大学 生物工程与食品学院，湖北 武汉 430068
Author(s):
 WANG Puzhao;  HE Shibo;  ZHAN Yifeng;  LIU Mingxing
 School of Biological Engineering and Food Science, Hubei Univ. of Tech., Wuhan 430068, China
关键词:
 ; 抗癌药物;  5-氟尿嘧啶-1-乙酰氯;  5-氟尿嘧啶;  化合物合成
Keywords:
 ; anti-cancer drugs;  5-fluorouracil-1-acetyl chloride; 5-fluorouracil; Compound synthesis
分类号:
R914.4
文献标志码:
A
摘要:
 以5-氟尿嘧啶为原料，经取代和酰基化反应合成目标化合物5-氟尿嘧啶-1-乙酰氯，探讨反应原料配比、温度和时间对各步产率的影响。这种抗癌药物关键中间体5-氟尿嘧啶-1-乙酰氯的合成新方法最佳工艺为：第一步反应中原料配比为1∶1.6，反应温度和时间分别为60℃和2 h；第二步反应中原料配比为1∶10，反应温度和时间分别为80℃和2 h。产物总收率达65.1%，并经1H-NMR分析表征。该合成工艺路线具有原料廉价易得、条件温和、操作简便等优点。
Abstract:
 A new synthetic method of 5-fluorouracil-1-acetyl chloride, a key intermediate of anticancer drugs, was reported. The target compound 5-fluorouracil-1-acetylchloride was synthesized from 5-fluorouracil by substitution and acylation reaction. The effects of raw material ratio, temperature and time on the yield of each step were discussed. The optimum process is as follows: in the first step, the ratio of raw materials is 1∶1.6, the reaction temperature and time are 60℃and 2 h respectively; in the second step, the ratio of raw materials is 1∶10, the reaction temperature and time are 80℃and 2 h respectively. The total yield of the product was 65.1%, which was characterized by 1H-NMR. The synthetic process has the advantages of cheap and easily available raw materials, mild conditions and simple operation.

参考文献/References:

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备注/Memo

备注/Memo:
［收稿日期］ 2021-10-14
［基金项目］ 国家级大学生创新创业训练计划项目（202010500019）
［第一作者］ 王溥照（2000-），男，湖北随州人，湖北工业大学本科生，研究方向为药物中间体的合成
［通信作者］ 刘明星（1970-），男，湖北武汉人，工学博士，湖北工业大学教授，研究方向为化学创新药物的合成与工艺
更新日期/Last Update: 2023-03-14