Synthesis of Phostones via the Palladium-Catalyzed Ring Opening of Epoxy Vinyl Phosphonates

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Abstract

The reaction of epoxy aldehydes with tetraethyl methylenediphosphonate gave γ,δ-epoxy vinyl phosphonates. The palladium-catalyzed addition of primary alcohols gave the monoprotected diols as single diastereoisomers. The  trans - and  cis -epoxides lead to opposite ( syn  and  anti ) diastereoisomers of the addition products. The alkene of the vinyl phosphonates was subjected to hydrogenation, and the resulting saturated phosphonates underwent base-catalyzed cyclization to give phostones with a very high diastereoselectivity in the formation of the new chiral center at the phosphorus atom.
Original languageAmerican English
JournalJournal of Organic Chemistry
Volume84
DOIs
StatePublished - May 29 2019

Disciplines

  • Physical Sciences and Mathematics
  • Chemistry
  • Organic Chemistry
  • Polymer Chemistry

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