[1]张嘉颖,裘京晓,黄程勇,等.抗癌药物马赛替尼的合成工艺优化[J].华侨大学学报(自然科学版),2019,40(2):215-220.[doi:10.11830/ISSN.1000-5013.201809018]
　ZHANG Jiaying,QIU Jingxiao,HUANG Chengyong,et al.Improved Synthesis of Anti-Cancer Drug Masitinib[J].Journal of Huaqiao University(Natural Science),2019,40(2):215-220.[doi:10.11830/ISSN.1000-5013.201809018]
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抗癌药物马赛替尼的合成工艺优化()
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《华侨大学学报（自然科学版）》[ISSN:1000-5013/CN:35-1079/N]

卷:
第40卷
期数:
2019年第2期
页码:
215-220
栏目:
出版日期:
2019-03-20

文章信息/Info

Title:
Improved Synthesis of Anti-Cancer Drug Masitinib
文章编号:
1000-5013(2019)02-0215-06
作者:
张嘉颖1;  裘京晓2;  黄程勇1;  吴振3;  王立强1
1. 华侨大学 生物医学学院, 福建 泉州 362021;2. 北京第二外国语大学 附属医院, 北京 100024;3. 厦门大学 药学院, 福建 厦门 361102
Author(s):
ZHANG Jiaying1;  QIU Jingxiao2;  HUANG Chengyong1;  WU Zhen3;  WANG Liqiang1
1. School of Biomedical Sciences, Huaqiao University, Quanzhou 362021, China; 2. Affiliated Hospital, Beijing International Studies University, Beijing 100024, China; 3. School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, China
关键词:
马赛替尼;  抗癌药物;  2-甲基-5-硝基苯胺;  工艺优化
Keywords:
masitinib;  anti-cancer drug;  2-methyl-5-nitroaniline;  optimization
分类号:
R944
DOI:
10.11830/ISSN.1000-5013.201809018
文献标志码:
A
摘要:
对现有文献报道的马赛替尼合成工艺进行优化改进.以2-甲基-5-硝基苯胺为原料,经缩合、噻吩环化、还原氢化、酰化等反应制备马赛替尼,产物结构经电喷雾质谱(ESI-MS),核磁共振氢谱(1H-NMR),核磁共振碳谱(13C-NMR)等确证,并对其中的合成条件进行优化对比研究.结果表明:优化工艺后,马赛替尼的总收率为37.3%(以2-甲基-5-硝基苯胺计),与文献报道的工艺相比,提高了9%;优化后的工艺具有反应时间短、成本低、收率高等特点,更易应用于工业化生产.
Abstract:
The synthesis process of masitinib which was reported in the literature was improved. Masitinib was synthesized by using 2-methyl-5-nitroaniline as a raw material, via condensation, cyclization, hydrogenation and acylation etc, its structure was confirmed by electrospray ionization mass spectrometry(ESI-MS), proton nuclear magnetic resonance(1H-NMR)and carbon 13 nuclear magnetic resonance(13C-NMR), and the reaction conditions of some steps were optimized. The results show that the yield of masitinib after optimization was up to 37.3%(in terms of 2-methyl-5-nitroaniline), which is 9% higher than that reported in literature; the optimized process has the characteristics such as short reaction time, low cost and high yield, and it’s easier to apply to industrial production.

参考文献/References:

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备注/Memo

备注/Memo:
收稿日期: 2018-09-10
通信作者: 王立强(1970-),男,教授,博士,主要从事药剂学和创新药物的研究.E-mail:wlq1599@163.com.
基金项目: 国家重点研发计划项目(2016YFE0101700); 华侨大学研究生科研创新能力培育计划资助项目(1701407 1021)
更新日期/Last Update: 2019-03-20