Abstract <p>(1<i>R</i>,5<i>S</i>)-2-Ethoxy-6,6-dimethyl-3-azabicyclo[3.1.0]hex-2-ene easily available from (+)-3-carene has been proposed as a key building block for the synthesis of Nirmatrelvir and related compounds. It has been obtained by enol ethylation of (1<i>R</i>,5<i>S</i>)-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2-one with triethyloxonium tetra­fluoroborate.</p>

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New Chiral Bicyclic Pyrrolidine Block for Nirmatrelvir and Its Analogues

  • G. R. Sunagatullina,
  • G. A. Shavaleeva,
  • Z. R. Valiullina,
  • M. S. Miftakhov

摘要

Abstract

(1R,5S)-2-Ethoxy-6,6-dimethyl-3-azabicyclo[3.1.0]hex-2-ene easily available from (+)-3-carene has been proposed as a key building block for the synthesis of Nirmatrelvir and related compounds. It has been obtained by enol ethylation of (1R,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2-one with triethyloxonium tetra­fluoroborate.