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An efficient method for the selective preparation of new CF3‐substituted α‐amino acid derivatives decorated with pharmacophore pyrimido[1,6‐a]indolone core has been developed via Rh(III)‐catalyzed C−H activation/[4+2]‐annulation of N‐(pivaloyloxy)‐indole‐1‐carboxamides with propargyl‐containing α‐amino carboxylates and α‐amino phosphonates. [ABSTRACT FROM AUTHOR]

A series of new orthogonally protected α‐CF3‐substituted α‐amino carboxylates, and α‐amino phosphonates decorated with pharmacophore isoquinolone core has been elaborated through the Rh(III)‐catalyzed C−H activation/annulation of aryl hydroxamates with propargyl‐containing α‐amino acid derivatives and their phosphorus analogues. [ABSTRACT FROM AUTHOR]

[Display omitted] An efficient and selective access to novel α-CF 3 -substituted γ,δ-didehydro lysine derivatives and their phosphorus analogues has been developed via the Cu-catalyzed Mannich reaction of α-amino α-propargyl α-trifluoromethyl carboxylates or phosphonates with different secondary amines and paraformaldehyde. [ABSTRACT FROM AUTHOR]

A convenient route to novel α-CF 3 -containing triazolyl α-amino acids and α-aminophosphonates with 3-alanyl substituent in heterocyclic moiety and distal OH-group, which can imitate the active elements of glutamate-based receptors, using Cu-catalyzed 1,3-dipolar cycloaddition of different α-azido acids and α-azido esters to functionalized acetylenes has been developed. [ABSTRACT FROM AUTHOR]

An efficient access to novel trifluoromethyl-substituted phosphonate analogues of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (TIC) derivatives based on regioselective rutheniumcatalyzed co-cyclotrimerization of functionalized 1,7-diynes with various alkynes has been developed using RuClCp"cod and preferably Grubbs second-generation catalysts. [ABSTRACT FROM AUTHOR]

Abstract: A convenient synthetic pathway to novel functionalized tetrapeptides containing the 1,2,3-triazole moiety is described. The target molecules were obtained by the reaction of fluorinated α-amino acids or α-aminophosphonates with azidopeptides via Cu(I)-catalyzed Huisgen cycloaddition reaction (click chemistry). The synthesized tetrapeptides may find important applications in biomedical chemistry as potential drugs. [Copyright &y& Elsevier]

Abstract: A convenient method for the preparation of α-CF3-α-aminophosphonates bearing alkynyl group at the α-carbon atom has been described. New alkynylphosphonates have been further utilized in the synthesis of functionalized triazole-containing α-CF3-α-aminophosphonates via copper-catalyzed (3+2)-cycloaddition to different organic azides. [Copyright &y& Elsevier]