铜促进的三氟甲基化反应研究进展.pdf

DOI: 10.6023/cjoc201311012 综述与进展 有机化学 Chinese Journal of Organic Chemistry REVIEW 铜促进的三氟甲基化反应研究进展 王光祖a 赫侠平a 戴建军*,a 许华建*,a,b (a 合肥工业大学医学工程学院 合肥 230009) (b 先进功能材料与器件安徽省重点实验室 合肥 230009) 摘要 药物分子中含有三氟甲基可以有效改善其亲脂性、可吸收性以及代谢稳定性. 因此, 在有机分子中引入三氟甲 基引起了人们的广泛关注. 近年来, 过渡金属催化的三氟甲基化反应得到了快速发展. 其中, 铜作为一种廉价且活性 较高的催化剂能够实现多种三氟甲基化反应. 从发生三氟甲基化反应的底物出发, 综述了近年来卤代烃、硼试剂、C— H 化合物、胺类、羧酸类化合物等的三氟甲基化反应研究进展. 关键词 铜催化; 三氟甲基化; 三氟甲基试剂 Recent Advances in Copper-Promoted Trifluoromethylation Reactions Wang, Guangzua He, Xiapinga Dai, Jianjun*,a Xu, Huajian*,a,b a ( School of Chemical Engineering, School of Medical Engineering, Hefei University of Technology, Hefei 230009) b ( Key Laboratory of Advanced Functional Materials and Devices, Anhui Province, Hefei 230009) Abstract Drug molecules that contain trifluoromethyl group can effectively improve their lipophilicity, absorbability and metabolic stability. Thus, considerable attention has been paid to the introduce of trifluoromethyl group into organic molecules. Recently, transition metal-catalyzed trifluoromethylation has been well developed. The cheap and high activity copper catalyst has also been used to access a variety of trifluoromethylation reactions. In this review, we focus the conv