Abstract
We report a facile and direct rhodium(III)-catalyzed allylation-intramolecular hydroamination sequence of 5-arylsubstituted pyrazoles with allyl methyl carbonate to deliver various 5,6-dihydropyrazolo[5,1–a]isoquinolines involving CH bond activation/cyclization process. This approach features good functional-group compatibility and complete regioselectivity. The detailed control experiments show that CH cleavage may be the rate-determining step.
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