Efficient synthesis of 4-substituted pyrazole via microwave-promoted Suzuki cross-coupling reaction

Pyrazoles and their derivatives are important heterocycles found in nature and present in numerous bioactive compounds. In contrast to 3 or 5-aryl pyrazole, the preparation of 4-aryl pyrazole is fairly rare. Utilizing microwave irradiation, the synthesis of 4-substituted-arylpyrazole via Suzuki cross-coupling has been developed with a wide range of substrates. The remarkable advantages of this method are mild reaction conditions, simple operation, high yield, and short reaction time. Product structures were identified by MS, 1H NMR, 13C NMR, and elemental analysis.

Graphical abstractUtilizing microwave irradiation, the synthesis of 4-substituted pyrazole via Suzuki cross-coupling has been developed with a wide range of substrates. The easy availability and the broad structural diversity of substrates make the reaction useful for the construction of 4-substituted pyrazole libraries.Figure optionsDownload full-size imageDownload as PowerPoint slide