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DICP OpenIR  > 中国科学院大连化学物理研究所  > 专利
学科主题: 物理化学
专利名称: 一种吡唑衍生物的制备方法;  一种吡唑衍生物的制备方法;  一种吡唑衍生物的制备方法;  一种吡唑衍生物的制备方法
作者: 余正坤1;  金伟伟1
申请受理号: CN201110031782.1
专利授权号: CN201110031782.1
申请日期: 2011-01-28
授权日期: 2014-12-03
专利权人: 中国科学院大连化学物理研究所
专利类别: 发明
是否PCT专利: 
授权日期: 2014-12-03
专利名称: 一种吡唑衍生物的制备方法;  一种吡唑衍生物的制备方法;  一种吡唑衍生物的制备方法;  一种吡唑衍生物的制备方法
公开日期: 2014-12-03
摘要: The invention discloses a method for preparing a pyrazole derivative and a tetra-substituted olefin (Z)-Tamoxifen which is a clinical drug for treating the breast cancer from a polysubstituted sulfo-olefin. The pyrazole derivative is prepared by carrying out a condensation cyclization reaction on a raw material alpha-oxoketone monothioacetal which is easy to prepare and has a structure diversity and various reaction centers and a nucleophilic reagent hydrazine at a reflux temperature; and the tetra-substituted olefin (Z)-Tamoxifen is prepared by carrying out a coupling reaction on the raw material alpha-oxoketone monothioacetal and arylboric acid at 50DEG under the catalysis of Pd. Compared with reported preparation methods of the pyrazole derivative and (Z)-Tamoxifen, the preparation method makes products have the advantages of good regioselectivity and stereoselectivity, easily available raw material, simple operation, mild preparation reaction conditions, and high efficiency. | 本发明公开了一种经由硫代多取代烯烃制备吡唑衍生物和治疗乳腺癌临床药物四取代烯烃(Z)-Tamoxifen的方法。在回流温度下,以易制备、具有结构多样性和多反应中心的α-羰基单硫缩烯酮为原料与亲核试剂肼进行缩合环化反应制备吡唑衍生物;在50℃与钯催化条件下,以α-羰基二硫缩烯酮为原料与芳基硼酸进行偶联反应制备四取代烯烃(Z)-Tamoxifen。与已报道的吡唑衍生物和(Z)-Tamoxifen的制备方法相比较,本发明产物区域选择性和立体选择性好、原料易得、操作简便、制备反应条件温和以及效率高。
内容类型: 专利
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/145267
Appears in Collections:中国科学院大连化学物理研究所_专利

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作者单位: 1.中国科学院大连化学物理研究所

Recommended Citation:
余正坤,金伟伟. 一种吡唑衍生物的制备方法, 一种吡唑衍生物的制备方法, 一种吡唑衍生物的制备方法, 一种吡唑衍生物的制备方法. CN201110031782.1. 2014.
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