4.4 Article

Enantioselective direct fluorination and chlorination of cyclic β-ketoesters mediated by phase-transfer catalysts

Journal

TETRAHEDRON LETTERS
Volume 54, Issue 21, Pages 2623-2626

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2013.03.028

Keywords

Fluorination; Chlorination; Phase-transfer catalysis (PTC); ketoesters

Funding

  1. National University of Singapore [R-143-000-469-112]
  2. Ministry of Education (MOE) of Singapore [R-143-000-362-112]
  3. GSK-EDB [R-143-000-491-592]

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A straightforward and practical method for the direct fluorination and chlorination of various beta-ketoesters employing a phase-transfer catalyst is developed. The desired products with fluorine/chlorine-substituted quaternary chiral centers are prepared with good to excellent enantioselectivities. (c) 2013 Elsevier Ltd. All rights reserved.

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