Synthesis of CF 3 -Containing Spiro-[Indene-Proline] Derivatives via Rh(III)-Catalyzed C-H Activation/Annulation.

Alexandra S BubnovaDaria V VorobyevaIvan A GodovikovAlexander F Smol'yakovSergey N Osipov

Published in: Molecules (Basel, Switzerland) (2023)

An efficient method of accessing new CF 3 -containing spiro-[indene-proline] derivatives has been developed based on a Cp*Rh(III)-catalyzed tandem C-H activation/[3+2]-annulation reaction of 5-aryl-2-(trifluoromethyl)-3,4-dihydro-2 H -pyrrole-2-carboxylates with alkynes. An important feature of this spiro annulation process is the feasibility of dehydroproline moiety to act as a directing group in the selective activation of the aromatic C-H bond.

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