Ligand-Promoted C(sp3)–H Olefination en Route to Multi-functionalized Pyrazoles

摘要

A Pd-catalyzed/N-heterocycle-directed C(sp³)–H olefination has been developed. The monoprotected amino acid ligand (MPAA) is found to significantly promote Pd-catalyzed C(sp³)–H olefination for the first time. Cu(OAc)2 instead of Ag⁺ salts are used as the terminal oxidant. This reaction provides a useful method for the synthesis of alkylated pyrazoles.