Study On Synthesis Of Aryl And Heteroaryl Trifluoromethyl Ketones

In recent years, the selectively fluorinated chemicals and their utilization have been greatly exploited in the rational design of new compounds with desired properties. Because the incorporation of fluorine atoms into organic compounds often leads to the significant modification of their biological and physiological activities, this strategy has been widely used in the design and optimization of biologically active molecules. As a typical fluorine-containing building block, the trifluoromethyl group is an essential structural motif in many biologically active compounds owing to its excellent metabolic stability, lipophilicity and electron-withdrawing in new pharmaceutical candidates.Schemel a two-step process for the synthesis of aryl and heteroaryl trifluoromethyl ketonesThis paper mainly presents a two-step process for the synthesis of aryl and heteroaryl trifluoromethyl ketones from the corresponding aldehydes. Trifluoro-methylated alcohols were prepared from aryl and heteroaryl aldehydes in excellent yields using catalytic amount of K2CO3. The trifluoromethyl carbinols were then oxidized conveniently and efficiently by o-iodoxybenzoic acid (IBX) under mild condition to get the desired functionalized aryl and heteroaryl trifluoromethyl ketones. These reactions demonstrate excellent reactivity, good functional group tolerance and high yields. Moreover, this procedure allows recycling and reuse of the oxidant. In the end, we also undertake a study on hand type substrates.