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

Christophe      Rochais; Sylvain      Rault; Patrick      Dallemagne

Abstract

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