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  • Title: Catalytic C-H allylation and benzylation of pyrazoles.
    Author: Bae S, Jang HL, Jung H, Joo JM.
    Journal: J Org Chem; 2015 Jan 02; 80(1):690-7. PubMed ID: 25517925.
    Abstract:
    We describe a general approach for the synthesis of allylated and benzylated pyrazoles. An electron-withdrawing substituent, such as nitro, chloro, and ester groups, at C4 renders the Lewis basic nitrogen atom to be less basic and the C-H bond more acidic than the ones of the parent ring, enabling Pd-catalyzed C-H allylation and benzylation reactions of pyrazoles. The new method expanding the scope of the C-H functionalization of pyrazoles beyond arylation reactions provides a rapid access to complex pyrazole compounds.
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