4.8 Article

A Cascade Phosphinoylation/Cyclization/Desulfonylation Process for the Synthesis of 3-Phosphinoylindoles

Journal

ORGANIC LETTERS
Volume 18, Issue 6, Pages 1242-1245

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b00056

Keywords

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Funding

  1. NSFC [21173178, 21232005, 21375113]
  2. National Basic Research Program of China [2012CB821600]
  3. Fundamental Research Funds for the Central Universities [20720160030]

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3-Phosphinoylindole derivatives play important roles as pharmaceutical drugs and ligands. A new method for the synthesis of 3-phosphinoylindole derivatives has been achieved through silver-mediated cycloaddition between N-Ts-2-alkynylaniline derivatives and H-phosphine oxides. This transformation offers a straightforward route to the formation of the C-P bond, indole ring, and desulfonylation in one step.

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