[1]童 航,詹一丰,何世波,等. 抗肿瘤药物培西达替尼关键中间体的合成[J].湖北工业大学学报,2023,(2):49-51.
　TONG Hang,ZHAN Yifeng,HE Shibo,et al. Synthesis of Key Intermediates of the Antitumor Drug Pexidartinib[J].,2023,(2):49-51.
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 抗肿瘤药物培西达替尼关键中间体的合成()
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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2期
页码:
49-51
栏目:
湖北工业大学学报
出版日期:
2023-04-30

文章信息/Info

Title:
 Synthesis of Key Intermediates of the Antitumor Drug Pexidartinib
文章编号:
1003-4684(2023)02-0049-03
作者:
 童 航;  詹一丰;  何世波;  王溥照;  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):
 TONG Hang; ZHAN Yifeng; HE Shibo; WANG Puzhao; LIU Mingxing
 School of Biological Engineering and Food，Hubei Univ. of Tech.，Wuhan 430068，China
关键词:
 ; 培西达替尼;  培西达替尼中间体;  抗肿瘤药物
Keywords:
 ; pexidartinib;  intermediate of pexidartinib;  antitumor drug;  chemical synthesis
分类号:
O626.32
文献标志码:
A
摘要:
 以6-氨基烟酸乙酯和6-三氟甲基烟醛为原料，合成抗肿瘤药物培西达替尼关键中间体(5-甲酰基吡啶-2-基){[6-(三氟甲基)吡啶-3-基]甲基}氨基甲酸叔丁基酯。整个工艺路线包括还原胺化、还原、氧化和取代，共4步反应，总收率达50.1%。各步产物经MS、1H NMR、13C NMR分析表征。该工艺路线具有原料廉价易得、反应条件温和、操作简便的优点，可望实现规模化生产。
Abstract:
 Tert butyl (5 formylpyridin 2 yl){[6-(trifluoromethyl)pyridine 3 yl]methyl}carbamate is used as the key intermediate of the anticancer drug pexidartinib. It was synthesized from 6 aminicotinic acid ethyl ester and 6 trifluoromethyl nicotinal as raw materials. The whole process includes reductive amination，reduction，oxidation and substitution，with a total yield of 50.1%. The products were characterized by MS， 1 H NMR and 13 C NMR. This process has the advantages of cheap raw materials，mild reaction conditions and simple operation，and is expected to achieve large-scale production.

参考文献/References:

[1] BENNER B，GOOD L，QUIROGA D，et al. Pexidartinib，a novel small molecule CSF-1R inhibitor in use for tenosynovial giant cell tumor: a systematic review of pre-clinical and clinical development[J]. Drug Design，Development and Therapy，2020，14: 1693-1704.
[2] 王宝林，王胜，李广乾，等. 一种吡昔替尼的简便制备方法[P]. CN: 201810144681.7，2019-08-23.
[3] 刘加艳，任宇鹏. 一种连续化生产pexidartinib的合成方法[P]. CN: 202010044798.5，2020-06-05.
[4] 李建其，陈东升，苏晓静. 用于制备派西尼布的中间体及其制备方法和应用[P]. CN: 201811562372.8，2020-06-30.
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备注/Memo

备注/Memo:
［收稿日期］ 2021-11-21
［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］ 童 航（1997-），男，湖北应城人，湖北工业大学硕士研究生，研究方向为新药研发
［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，研究方向为新药研发
更新日期/Last Update: 2023-04-26