Enantioselective γ‐addition of pyrazole and imidazole heterocycles to allenoates catalyzed by chiral phosphine

Chiral phosphine were found to catalyze the enantioselective asymmetric γ‐addition of heteroaromatic compounds to allenoates in good yields with high enantiomeric ratios and regio‐selectivities in the presence of (S)‐BINOL. Both pyrazole and imidazole could be employed in this process. The synthetic value of these γ‐addition products was demonstrated by the preparation of biologically relevant molecules and structural scaffolds. Remarkably, the synthetic utility of this strategy was demonstrated through a two‐step synthesis of JAK inhibitor.

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