二氟甲基化方法研究进展

doi:10.6023/cjoc201801041

摘要/Abstract

二氟甲基官能团（CF₂H）具有强的亲脂性和吸电子性，能显著增强有机分子的生理活性.含CF₂H的分子在药物、农药等领域的应用研究已受到人们的极大关注.因此，如何简便、高效地向分子中引入CF₂H基团成为当前有机氟化学领域的一个研究热点.近年来，新的二氟甲基化试剂及官能化方法得到了快速发展，为研究者提供了较为丰富的引入CF₂H的手段.针对不同结构分子的二氟甲基化，对近年来发展的高效二氟甲基化试剂及二氟甲基化过程涉及的新反应、新催化剂及反应机理做着重介绍，最后将对二氟甲基化领域存在的问题和难点进行简要的展望.

关键词: 二氟甲基, 亲核试剂, 亲电试剂, 二氟卡宾, 直接二氟甲基化

The difluoromethyl functional group (CF₂H) which has strong lipophilic and electron-withdrawing properties can significantly enhance the physiological activity of organic molecules. The applications of CF₂H-containing compounds in the fields of drugs, agrochemicals and so on have attracted great attention of many research groups. Therefore, the development of effective and general methodologies for the selective incorporation of difluoromethyl groups has become one of the hotspots in the field of organic chemistry. Recently, new difluoromethylation reagents and methods that were able to efficiently incorporate the difluoromethyl group under mild conditions have been developed rapidly, that pave the way for the facile introduction of difluoromethyl group into site-specific positions of the target molecules. In this paper, we will first briefly introduce some organic molecules with different functional groups which can be difluoromethylated, and then focus on the development of the recent high-performance difluoromethylation reagents, new reactions and catalysts. Finally, we will discuss the remaining problems and challenges in this particular field.

Key words: drifluoromethyl, nucleophilic reagent, electrophilic reagent, difluorocarbene, direct difluoromethylation

引用此文

王为强, 余秦伟, 张前, 李江伟, 惠丰, 杨建明, 吕剑. 二氟甲基化方法研究进展[J]. 有机化学, 2018, 38(7): 1569-1585.

Wang Weiqiang, Yu Qinwei, Zhang Qian, Li Jiangwei, Hui Feng, Yang Jianming, Lü Jian. Recent Progress on Difluoromethylation Methods[J]. Chin. J. Org. Chem., 2018, 38(7): 1569-1585.

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