论文部分内容阅读
三氟甲硫基脂溶性高、吸电子能力强,将其引入药物分子中可以改变分子药代动力学以及物理化学特性,提高代谢稳定性.含三氟甲硫基的分子在医药、农药、材料以及含氟日用品等领域得到了广泛的应用.因此,如何高效地向分子中引入三氟甲硫基团成为了近些年来有机氟化学领域的一个研究热点.经过几年的研究,新的三氟甲硫基化试剂及方法得到了快速的发展,为药物化学家提供了方便简洁地引入三氟甲硫基团的工具箱.在本篇综述中,将首先简要介绍间接引入三氟甲硫基团的方法,随后将对直接引入三氟甲硫基团的方法,尤其是近些年来发展的过渡金属催化、亲电三氟甲硫基化以及自由基类型的三氟甲硫基化方法做着重的介绍.最后将对三氟甲硫基化领域存在的问题和难点进行简要的展望.
Trifluoromethylthio lipid has high solubility and strong electron-withdrawing ability, which can change the molecular pharmacokinetics and physicochemical properties of the drug, and improve the metabolic stability. Materials and fluorine-containing daily necessities, etc. Therefore, how to introduce trifluoromethylsulfide into the molecule efficiently has become a research hotspot in the field of organofluorine chemistry in recent years.After several years of research, the new Trifluoromethylthioating reagents and methods have been rapidly developed, providing chemotherapists with a convenient and concise toolbox for the introduction of trifluoromethylthio groups.In this review, we will first briefly introduce the indirect introduction of trifuroxine Sulfur group, followed by a direct introduction of the trifluoromethylthio group, in particular the transition metal-catalyzed, electrophilic trifluoromethylthiolation and free radical-type trifluoromethylthiolation developed in recent years Method is introduced emphatically.Finally, the problems and difficulties in the field of trifluoromethylthiourea will be briefly discussed.