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Intramolecular Cyclisation of β-Aryl-β-Amino Acids in the Design of Novel Heterocyclic Systems with Therapeutic Interest: An Unfailing Source of Diversity

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β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their application in the medicinal chemistry field.

Keywords: -Phenylalanine; -aryl--amino acids; -ketoesters; -peptides; 3-amino-3-arylpropionic Acids; AROMATIC RING; Aminoindanones; Aryl-Aza Six-Membered Rings; Aryl-Pyrimidines; Aryl-Thiazines; Aryloxazines; Aster tataricus; CBr4; CC moiety; CCR5 receptor antagonist; CCl4; CYCLISATION; CeCl3; DIEA; EtOAc; Gram-positive bacteria; HIV-1; Heterocyclic; Heterocyclic Isosters; Hydrolysis; Intramolecular Cyclisation; Jaspamide; Maytenus mossambicensis; Microsporum canis; Mukaiyama's reagent; N-alkylated; N-methylated; NaBH4; Nodularin; Ohno's method; OsO4; PP2A; Piperazines; Piperidines; Plasmodium falciparum; Pyrimidines; SAR; Schiff bases; TFA; Triphenylphosphine; VMAT2; alcohol; amino groups; aminoisoquinolones; ammonia; aromatic -amino acids; aromatic ring; astins; azetidinones; bleomycins; carboxylate group; carboxylic acid group; cyclodehydration; cytotoxic activity; diazo compounds; ethyl carboxylate; ezetimibe; hydrogenation; hydroxyl group; iminium salts; isonitriles; ligand; maraviroc; methanesulfonyl chloride; microcystin; monocarbon; oxazetidinylacetamides; oxopyrrolidinyl carboxylates; pesticidal; phosphonates; pyrrolidinedione ring; racemic; rhodium; rhodium acetate; stereoselective; toxins; β-aryl-β-amino acids

Document Type: Research Article


Publication date: December 1, 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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