A convenient catalytic protocol for the synthesis of electron-poor indoles was envisioned. A cyclisation reaction of electron-deficient 2-(alkynyl)-anilines, catalysed by Zn(II) salts, was successfully developed and applied to the synthesis of an API precursor. A two-step one-pot procedure starting from aniline derivatives was successfully developed. The use of a readily available, non-noble metal further enhanced the value of the protocol.
A convenient protocol for a zinc-catalysed synthesis of electron-poor indoles / F. Medici, F. Montinari, E. Donato, L. Raimondi, M. Benaglia. - In: TETRAHEDRON LETTERS. - ISSN 0040-4039. - 116:(2023 Feb 17), pp. 154340.1-154340.4. [10.1016/j.tetlet.2023.154340]
A convenient protocol for a zinc-catalysed synthesis of electron-poor indoles
F. Medici
Primo
;E. Donato;L. RaimondiPenultimo
;M. Benaglia
Ultimo
2023
Abstract
A convenient catalytic protocol for the synthesis of electron-poor indoles was envisioned. A cyclisation reaction of electron-deficient 2-(alkynyl)-anilines, catalysed by Zn(II) salts, was successfully developed and applied to the synthesis of an API precursor. A two-step one-pot procedure starting from aniline derivatives was successfully developed. The use of a readily available, non-noble metal further enhanced the value of the protocol.
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revised Te Lett.pdf
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