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Keywords:

  • asymmetric catalysis;
  • cyclization;
  • indoles;
  • Michael addition;
  • phase-transfer catalysis
Thumbnail image of graphical abstract

Producing polycycles: A mild and direct stereocontrolled route to pharmacologically active pyrazino-indol-1-ones has been developed. The optimal phase-transfer conditions provide variously functionalized ring-closed compounds in high chemical and optical yields (see scheme; X=H, F, Cl, Me, OMe; Ar=Ph, β-naphthyl; R′=tBu, Et, Me; R=benzyl, para-methoxyphenyl).