Consequently, introduction of SCF3 group to chromones might be very desirable and result in further advances in the pharmacological applications. Recently, Yang and co-workers first demonstrated a facile and general synthetic route to a range of 3-((trifluoromethyl)thio) chromones via in situ generation of electrophilic trifluoromethylthio species from trichloroisocyanuric acid (TCCA) and AgSCF3 on Organic Letters.
This practical and easily handled reaction, which was insensitive to air and moisture, could occur under mild conditions in a short reaction time without any extra additives. Moreover, the reaction could be scaled-up easily. Additionally, this approach could be applied in construction of (trifluoromethyl)thio-containing analogue of natural topopyrone C.(The link to the article: http://pubs.acs.org/doi/abs/10.1021/ol502751k )
This work was financially supported by the Chinese Academy of Sciences (“Interdisciplinary Cooperation Team” Program for Science and Technology Innovation), the National Natural Science Foundation of China (81321092), and SKLDR/SIMM (SIMM1403ZZ-01).
In addition, Yang’s group did a lot of research on the application of 2-Acetylphenol, including the synthesis of a series of privileged structures in medicinal chemistry such as 2‑aminopyrroles/pyridines(Org. Lett.,2014,16,4186)、α-carbolines(Org. Biomol. Chem.,2014,12,355)、pyridinefused coumarins(RSC. Adv.,2013,3,5807)、2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones(RSC. Adv., 2013,3,35807)、pyrazole-containing bisphosphonate esters(Org. Biomol. Chem.,2012,10,7730)etc. What’s more, cooperating with Miao’s group, they found two (YCH337 and YCH665) of those compounds could inhibit both tubulin and topoisomerase II at very low (nanomolar) concentration and further studies of this series of compounds are in progress.
