Al-Bogami Abdullah S, Saleh Tamer S, Albishri Hassan M
Chemistry Department, Faculty of Science, King Abdulaziz University, North Jeddah, P,O box 80203, Jeddah 21589, Saudi Arabia.
Chem Cent J. 2013 Jun 13;7(1):101. doi: 10.1186/1752-153X-7-101.
Most of the known approaches to the synthesis of CF3-containing organic compounds suffer from serious drawbacks. For example the starting materials required for these methods are rather difficult to obtain, or they are fairly toxic and inconvenient to work with and methods for direct fluorination and trifluoromethylation do not always allow the introduction of the CF3-group at the required position of a molecule.
An efficient and attractive regioselective synthesis of a series of novel pyrazoles containing the trifluromethyl moiety was achieved using Cu(OTf)2/Et3N as an efficient catalytic system under ultrasonic irradiation.
Cu(OTf)2/Et3N catalyst showed a great advantage over all the investigated catalysts, and the ultrasonic irradiation method offered high yields of pyrazoles in short reaction time compared with classical conditions. gHMBC spectra of the product were used to rationalize the observed regioselectivity.
大多数已知的含CF3有机化合物的合成方法都存在严重缺陷。例如，这些方法所需的起始原料相当难以获得，或者它们毒性较大且操作不便，并且直接氟化和三氟甲基化方法并不总是能使CF3基团引入到分子的所需位置。
以Cu(OTf)2/Et3N作为高效催化体系，在超声辐射下实现了一系列含三氟甲基部分的新型吡唑的高效且有吸引力的区域选择性合成。
Cu(OTf)2/Et3N催化剂相较于所有研究的催化剂显示出巨大优势，并且与传统条件相比，超声辐射方法在短反应时间内提供了高产率的吡唑。产物的gHMBC光谱用于解释观察到的区域选择性。
