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科技导报 |研究论文 2012 , 30 (5) : 49 -51
癌症治疗药物埃罗替尼的合成
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王险1, 宋芳2, 冯清伟1
作者信息
    1. 国家知识产权局专利审查协作中心化学处,北京 100083;2. 中牧研究院,北京 102206
The Synthesis of Cancer Treatment Medicine Erlotinib
  • WANG Xian1, SONG Fang2, FENG Qingwei1
  • Affiliations
      1. Chemistry Division of Patent Examination Cooperation Center, State Intellectual Property Office of the People's Republic of China, Beijing 100083, China;2. China Animal Husbandry Institute, Beijing 102206, China
    出版时间: 2012-02-18 doi: 10.3981/j.issn.1000-7857.2012.05.007
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    提供了一种埃罗替尼的制备方法,该方法以3,4-二羟基苯甲酸乙酯为起始原料,经过与乙二醇单甲醚的醚化反应,再经硝化、还原、缩合成环,然后经卤化与间氨基苯乙炔反应,最后通入干燥的氯化氢气体后生成埃罗替尼。其中,硝化工艺相比于以前的工艺有较大的改进。本合成路线具有反应条件温和、总收率好、后处理简便易行和易于进行工业化生产等优点。
    埃罗替尼  /  硝化  /  合成
    The concise synthesis of Erlotinib was described. Treatment of Ethyl 3,4-dihydroxybenzoate with 2-methoxyethyl methanesulfonate followed by nitration, reduction, cyclization and chloration to afford 4-chloro-6,7-bis(2-methoxyethoxy)-1,4-dihydroquinazoline, which was treated with 3-ethynylaniline and then with dry hydrochloride to give Erlotinib. In this synthesis, the nitration process has greatly been improved. The advantages of this synthetic route include short reaction time, good total yield, and simple work-up.
    Erlotinib  /  nitration  /  synthesis
    王险;宋芳;冯清伟. 癌症治疗药物埃罗替尼的合成. 科技导报, 2012 , 30 (5) : 49 -51 . DOI: 10.3981/j.issn.1000-7857.2012.05.007
    WANG Xian;SONG Fang;FENG Qingwei. The Synthesis of Cancer Treatment Medicine Erlotinib[J]. Science & Technology Review, 2012 , 30 (5) : 49 -51 . DOI: 10.3981/j.issn.1000-7857.2012.05.007

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    doi: 10.3981/j.issn.1000-7857.2012.05.007
    • 接收时间:2011-08-31
    • 首发时间:2012-02-18
    • 出版时间:2012-02-18
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    • 修回日期:2012-01-15
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    2种不同金属材料的力学参数

    Family
    属数
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    Number of
    species
    占总种数比例
    Percentage of
    total species (%)

    Genus
    种数
    Number of
    species
    占总种数比例
    Percentage of total
    species (%)
    鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
    小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
    多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
    红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
    小菇属 Mycena 11 5.26
    光柄菇属 Pluteus 5 2.39
    红菇属 Russula 17 8.13
    栓菌属 Trametes 5 2.39
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