Zhao Haiwei, Gu Yang, Shen Qilong
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, P. R. China.
Chem Rec. 2023 Sep;23(9):e202300124. doi: 10.1002/tcr.202300124. Epub 2023 May 17.
Due to its unique physical and electrophilic properties, the difluoromethyl group (-CF H) has been playing an irreplaceable role in the field of pharmaceutical and agrochemical industry. Methods that could efficiently incorporate the difluoromethyl group into the target molecules are increasing in the recent years. Developing a stable and efficient difluoromethylating reagent is thus highly attractive. In this review, we describe the development of a nucleophilic difluoromethylation reagent [(SIPr)Ag(CF H)], including its elemental reaction, difluoromethylation reaction with different types of electrophiles, and its application in the synthesis of a nucleophilic and an electrophilic difluoromethylthiolating reagent.
由于其独特的物理和亲电性质,二氟甲基(-CF₂H)在制药和农用化学品工业领域一直发挥着不可替代的作用。近年来,能够将二氟甲基有效地引入目标分子的方法不断增加。因此,开发一种稳定且高效的二氟甲基化试剂极具吸引力。在本综述中,我们描述了亲核二氟甲基化试剂[(SIPr)Ag(CF₂H)]的发展,包括其基本反应、与不同类型亲电试剂的二氟甲基化反应,以及其在亲核和亲电二氟甲基硫醇化试剂合成中的应用。