A convenient route to 4-phenyl-5-aminothiazoles is described, which offers control over substitution at the 2-position. 2-N-Acylglycinamides were dithionated and a subsequent TFAA-mediated cyclisation step was followed by removal of the 5-N-trifluoroacetyl group providing the free amines. Though applicable generally the method was found to be most effective when introducing aromatic substituents at the 2-position, whereupon moderate overall yields of the 5-amino compounds were obtained. © 2006 Elsevier Ltd. All rights reserved.
CITATION STYLE
Thompson, M. J., Heal, W., & Chen, B. (2006). Synthesis of 5-aminothiazoles as building blocks for library synthesis. Tetrahedron Letters, 47(14), 2361–2364. https://doi.org/10.1016/j.tetlet.2006.02.004
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