Only very limited methods are available for the synthesis of 5-amino imidazoles. We report in this paper that three-component reaction of acyl chlorides, carbodiimides and α-isocyanoacetates or TosMIC took place smoothly in the presence of Et 3 N (2.5 equiv.) and a catalytic amount of copper iodide (0.2 equiv.) to afford 1,4-disubstituted 5-acetamidoimidazoles in good yields.
Novel Approach to the Synthesis of Aliphatic and Aromatic α-Keto Acids. -1,4-Diacetylpiperazine-2,5-dione is used in the reaction with the aromatic and aliphatic aldehydes to afford the aldol intermediates with complete (Z)-selectivity. Hydrolysis of the latter products leads to the target α-keto acids [cf. (IV), (VII)]. No keto acids are formed in the case of the heteroaromatic products with the exception of 2-thiophenyl derivative (IVe). -(BALDUCCI, D.; CONWAY, P. A.; SAPUPPO, G.; MUELLER-BUNZ, H.; PARADISI*, F.; Tetrahedron 68 (2012) 36, 7374-7379, http://dx.
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