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https://doi.org/10.1002/ejoc.201301734
Copy DOIPublication Date: Feb 3, 2014 | |
Citations: 35 |
AbstractAn efficient protocol for the direct CH‐functionalization of indole and its derivatives has been developed by using Cu(F3‐acac)2‐catalyzed insertion of CF3‐carbene derived from methyl 3,3,3‐trifluoro‐2‐diazopropionate. The reaction proceeds with high regioselectivity within a few minutes under low catalyst loading and allows the introduction of CF3 and carboxylate functions simultaneously into the 3‐ or 2‐position of the indole core. This method can be successfully applied for the synthesis of trifluoromethyl‐containing paullones, which are new members of the known family of potent inhibitors of cyclin‐dependent kinases.
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