Tolstoluzhsky Nikita V, Gorobets Nikolay Yu, Kolos Nadezhda N, Desenko Sergey M
Department of Organic Chemistry, V. N. Karazin Kharkiv National University, Svobody Square, 4, Kharkiv 61077, Ukraine.
J Comb Chem. 2008 Nov-Dec;10(6):893-6. doi: 10.1021/cc800103f. Epub 2008 Aug 21.
The derivatives of 4-(hetero)aryl-4-oxobut-2-enoic acid are useful as building blocks in the synthesis of biologically active compounds. An efficient general protocol for the synthesis of these building blocks was developed. This method combines microwave assistance and ytterbium triflate catalyst and allows the fast preparation of the target acids starting from different (hetero)aromatic ketones and glyoxylic acid monohydrate giving pure products in 52-75% isolated yields.