【摘 要】
：
由于CF2基团的特点,在分子中引入CF2有可能明显性质或者增强生理活性,因此在分子中引入CF2基团是提高药物性能的一种可选途径,通常的引入CF2的方法有直接氟化法和含氟砌
【机 构】
：
上海大学化学系,上海200444上海大学化学系,上海200444;中科院上海有机所,氟化学重点实验室
【出 处】
：
中国化学会第十三届全国有机合成化学学术研讨会
论文部分内容阅读
由于CF2基团的特点,在分子中引入CF2有可能明显性质或者增强生理活性,因此在分子中引入CF2基团是提高药物性能的一种可选途径,通常的引入CF2的方法有直接氟化法和含氟砌块法和含氟砌块法.直接氟化法往往需要昂贵、有毒的试剂,而含氟砌块法则通常条件温和操作简便.二氟溴乙酸乙酯作为一种商品化的廉价的含氟砌块[1],将其用于合成CF2的物质,可以节约成本提高效率.2015年施敏课题组[2]用苯基亚甲基环丙烷衍生物和三氟甲基化试剂通过铜催化的自由基机理反应得到了含CF3的1,2-二氢萘衍生物.张新刚课题组[3]用二氟溴乙酸乙酯在钯催化条件下得到了一系列含氟的苯乙烯衍生物.本文在此基础之上,使用二氟溴乙酸乙酯,通过自由基机理制备了一系列含二氟甲基的1,2-二氢萘的衍生物(Scheme 1),目前该项工作仍在继续中.
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