Goikhman R1, Jacques TL, Sames D.
J Am Chem Soc. 2009 Mar 4;131(8):3042-8. doi: 10.1021/ja8096114.Pyrazoles are important azole heteroarenes frequently found in pharmaceuticals and protein ligands, and there has been a growing interest in new synthetic methods for their preparation. We report the first catalytic intermolecular C-H arylation of pyrazoles, namely SEM-protected pyrazoles and N-alkylpyrazoles, which lays the foundation for a new approach to the synthesis of complex arylated pyrazoles, where new arene rings are directly attached to predetermined positions of the heteroarene nucleus ("topologically obvious synthesis"). Read More