An efficient method of accessing new CF3-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-2H-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.
An efficient access to the novel representatives of α,α-disubstituted α-amino acids with 1,3-enyne unit located at their side chain has been elaborated. The method is based on Pd(II)-catalyzed hydroalkynylation of α-allenyl-α-dimethylamino esters with terminal acetylenes. The developed strategy is the first example of the metal-catalyzed allene-alkyne coupling to provide a convenient route to new unsaturated α-amino acid derivatives in good yields and high selectivity.
14 October 2026 in Organic & Biomolecular Chemistry
A regioselective pathway to new fluorinated γ-arylated α-amino acid derivatives bearing a terminal double bond in the side chain has been developed based on Pd-catalyzed allene hydroarylation using ArI and TsNHNH 2 as aryl and hydride sources.