4.4 Article

A novel and convenient strategy for the synthesis of phthalazines from an aryne precursor

Journal

TETRAHEDRON LETTERS
Volume 54, Issue 51, Pages 7056-7058

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2013.10.075

Keywords

Phthalazine; Aryne; Pyridazine; Diaza-Wittig

Funding

  1. IWT (Agentschap voor Innovatie door Wetenschap en Technologie) [90704]
  2. Galapagos NV [90704]

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A novel three-step entry toward phthalazine derivatives has been elaborated. A strategy based on a sequential acyl-alkylation/diazo transfer reaction/Diaza-Wittig reaction led to the desired analogues in moderate to good yields from an aryne precursor. Various aryl groups were introduced on the annulated pyridazine, moreover the presence of an ester group allows further modifications. (C) 2013 Elsevier Ltd. All rights reserved.

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