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Keywords:

  • aldol reaction;
  • asymmetric catalysis;
  • atorvastin;
  • thioamides;
  • total synthesis
Thumbnail image of graphical abstract

An efficient enantioselective synthetic route to atorvastatin was developed based on a direct catalytic asymmetric aldol reaction. The expensive chiral ligand used in the initial aldol reaction was readily recovered (91 %) and reused. Implementation of an oxy-Michael reaction for the construction of the syn-1,3-diol unit eliminated several redundant steps, allowing for rapid access to the common intermediate in six steps (see scheme).