1609979-82-9Relevant articles and documents
Cu-catalyzed carbenoid functionalization of indoles by methyl 3,3,3-trifluoro-2-diazopropionate
Tsyshchuk, Irina E.,Vorobyeva, Daria V.,Peregudov, Alexander S.,Osipov, Sergey N.
, p. 2480 - 2486 (2014/05/06)
An 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. An efficient Cu-catalyzed direct CH-functionalization of indoles with methyl 3,3,3-trifluoro-2-diazopropionate has been developed. The reactions proceed within a few minutes under low catalyst loading to give the corresponding C3 or C2 substitution products with high regioselectivity. This method has been successfully applied for the synthesis of trifluoromethyl-containing paullone. Copyright
